bile acid, usually conjugated with either glycine or taurine; acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine.


An essential nutrient and natural water-soluble vitamin of the B-complex family that must combine with an intrinsic factor for absorption by the intestine, Vitamin B12 (cyanocobalamin) is necessary for hematopoiesis, neural metabolism, DNA and RNA production, and carbohydrate, fat, and protein metabolism. B12 improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. B12 metabolism is interconnected with that of folic acid. Vitamin B12 deficiency causes pernicious anemia, megaloblastic anemia, and neurologic lesions.


A synthetic mast cell stabilizer with anti-inflammatory activity. Cromolyn probably interferes with the antigen-mediated calcium ion influx into mast cells. This prevents mast cell degranulation, resulting in mast cell stabilization and inhibition of the release of inflammatory mediators, such as histamine and leukotrienes, which are involved in type I allergic reactions. Cromolyn also prevents inflammatory mediator release from eosinophils.


bile acid formed by bacterial action from cholate; usually conjugated with glycine or taurine; deoxycholate acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.


An analogue of the hormone vasopressin with antidiuretic and antihemorrhagic properties. Desmopressin acetate has selective affinity for the V2 receptor and acts on the distal kidney tubule by increasing the cellular permeability thereby stimulating water reabsorption. This antidiuretic agent is used in the treatment of central diabetes insipidus. An unrelated action of desmopressin acetate is to increases circulating factor VIII and is used in patients with haemophilia and von Willebrand's disease.


group of glucose polymers made by certain bacteria; dextrans are used therapeutically as plasma volume expanders and anticoagulants; they are also commonly used in biological experimentation and in industry for a wide variety of purposes.


A sulfhydryl-containing carbamate that is the primary in vivo metabolite of disulfiram. Diethyldithiocarbamate chelates zinc, thereby inhibiting metalloproteinases, thereby preventing the degradation of the extracellular matrix and inhibiting an initial step in cancer metastasis and angiogenesis. A known inhibitor of superoxide dismutase, this agent can either potentiate or protect against cell oxidative damage caused by ionizing radiation, depending on the time of administration. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C432" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C432" NCI Thesaurus)


The tartrate salt form of ergotamine, an ergot alkaloid and adrenergic alpha agonist with vasoconstrictor activity. Ergotamine tartrate selectively binds to alpha-adrenergic receptors thereby stimulating vascular smooth muscle and causing vasoconstriction in both arteries and veins. Ergotamine tartrate also blocks serotonin 5-HT1D receptors, thereby also causing vasoconstriction in cerebral blood vessels. Constriction of cerebral blood vessels caused by this agent may reduce the blood flow and pressure in cerebral arteries and may relieve the pain of vascular headaches.


ethane-1-hydroxy-1,1-diphosphonate; a diphosphonate compound that affects calcium metabolism and inhibits the resorption and deposition of hydroxyapatite crystals in bone.


The acetate salt form of flecainide, a synthetic agent derived from trifluoroethoxy-benzamide exhibiting antiarrhythmic and local anesthetic activity. As a class Ic antiarrhythmic that blocks sodium channels, flecainide depresses polarization phase 0 and decreases the induction velocity of the His-Purkinje system. It also decreases phase 4 slope and increases the depolarization threshold.


A group of substances similar to VITAMIN K 1 which contains a ring of 2-methyl-1,4-naphthoquinione and an isoprenoid side chain of varying number of isoprene units. In vitamin K 2, each isoprene unit contains a double bond. They are produced by bacteria including the normal intestinal flora.


The nitrate salt form of miconazole, an antifungal synthetic derivative of imidazole and used in the treatment of candidal skin infections, Miconazole selectively affects the integrity of fungal cell membranes, high in ergosterol content and different in composition from mammalian cells membranes. (NCI04)


The maleate salt form of timolol, a propanolamine derivative and a non-selective beta-adrenergic antagonist with antihypertensive property. Timolol competitively binds to beta-1-adrenergic receptors in the heart and vascular smooth muscle and beta-2-receptors in the bronchial and vascular smooth muscle, resulting in a decrease in beta-adrenergic stimulation. Beta-1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta-2-blockade results in an increase in peripheral vascular resistance. The ultimate results include vasodilation, and negative chronotropic and inotropic effects. In addition, timolol reduces intra-ocular pressure possibly by decreasing aqueous humor production by reduction of blood flow to the ciliary processes and cAMP synthesis.


The sodium salt form of tolmetin, an arylalkanoic acid and non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic activities. Although the exact mechanism through which tolmetin exerts its effects has yet to be fully elucidated, this agent appears to inhibit the enzyme prostaglandin synthase. This prevents the formation of prostaglandins from prostaglandin precursors, including the synthesis of the inflammatory prostaglandin E2 (PGE2) from the precursor prostaglandin H2 (PGH2). This prevents prostaglandin-mediated effects, including pain, inflammation and fever.


A compound containing vitamin A, a natural, fat-soluble vitamin that plays a vital role in a variety of physiologic processes including immune function, vision, reproduction, and cellular growth and differentiation. Upon administration, the various forms of vitamin A are solubilized into micelles in the intestinal lumen and absorbed by duodenal mucosal cells.


VITAMIN B 6 refers to several PICOLINES (especially PYRIDOXINE; PYRIDOXAL; & PYRIDOXAMINE) that are efficiently converted by the body to PYRIDOXAL PHOSPHATE which is a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, and aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into PYRIDOXAMINE phosphate. Although pyridoxine and Vitamin B 6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading (EE Snell; Ann NY Acad Sci, vol 585 pg 1, 1990). Most of vitamin B6 is eventually degraded to PYRIDOXIC ACID and excreted in the urine.


An amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. Fatty acids are utilized as an energy substrate in all tissues except the brain. (NCI04)


A radioactive salt that is used as a reagent in the preparation of indium 111-labeled radiopharmaceuticals. Indium 111-labeled radioconjugates are used as radioactive tracers in nuclear medicine that detect malignant lesions and inflammatory tissues probably due to an increased capillary permeability. Indium-111 chloride is particularly used in the radiolabeling of the monoclonal antibodies satumomab pendetide, 7E11-C5.3 (CYT-356), and ibritumomab tiuxetan. (NCI05)


A four carbon linear hydrocarbon that has a hydroxy group at position 1.


A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.


An adenine arabinonucleoside derivative that acts as an antineoplastic antimetabolite. It is used in the treatment of ACUTE LYMPHOID LEUKEMIA in pediatric patients who have relapsed.


An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia.


A cholinergic analogue with glandular secretion stimulatory activity. Cevimeline binds to and activates muscarinic receptors, thereby increasing the secretions in exocrine salivary and sweat glands. This cholinergic agonist also increases the tone of smooth muscle in the gastrointestinal and urinary tracts. Cevimeline is being studied as a treatment for dry mouth caused by radiation therapy to the head and neck.


A sunscreen blocker. Avobenzone is a topical, broad range UV protector and blocks UVA I, UVA II, and UVB wavelengths, thereby limiting the impact of UV rays on skin. (NCI05)


The propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.


A nonhormonal medication for the treatment of postmenopausal osteoporosis in women. This drug builds healthy bone, restoring some of the bone loss as a result of osteoporosis.


The hydrochloride salt of alfuzosin, a quinazoline compound with smooth muscle-relaxing activity. Alfuzosin selectively binds to and antagonizes post-synaptic alpha-1-adrenoreceptors in smooth muscle of the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra, initiating relaxation of smooth muscle and resulting in improvement of urine flow and the symptoms of benign prostatic hyperplasia (BPH). This agent also blocks alpha-1-adrenoreceptors in peripheral vascular smooth muscle, resulting in vasodilatation and a decrease in peripheral vascular resistance.


marine algal polysaccharide; used as dental impression material.


The oil extracted from the seed fruits of Prunus amygdalus. Almond oil is typically used as a skin emollient and for massage.


A compound with the chemical formula AlCl3; the anhydrous salt is used as a catalyst in organic chemical synthesis, and hydrated salts are used topically as antiperspirants, and for the management of HYPERHYDROSIS.


The aluminum salt of the fatty acid, stearic acid.


A benzamide derivative that is used as an antipsychotic agent for the treatment of schizophrenia. It is also used as an antidepressive agent.


An anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.


The active metabolite of benazepril, a carboxyl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Once the prodrug benazepril is metabolized to benazeprilat in the liver, benazeprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II, resulting in vasodilation. Benazeprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


The oil extracted from the fruit peel of Citrus bergamia. Bergamot oil is used in the treatment of psoriasis, mycosis fungoides, and vitiligo. Additionally, it is used as a citrus flavoring agent.


A synthetic quaternary ammonium base derivative, parasympathomimetic Bethanechol is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Generally used to increase smooth muscle tone, Bethanechol is used to treat reflux esophagitis and to initiate urination after surgery, in urinary infections, or for enlarged prostate. It may cause hypotension, cardiac rate changes, and bronchial spasms. (NCI04)


A mineral compound that is used to treat duodenal and gastric ulcers associated with Helicobacter pylori.


The mesylate salt of bitolterol, a diester sympathomimetic amine with bronchodilator activity. As an ester prodrug, bitolterol is hydrolyzed by esterases to its active metabolite colterol (N-t-butylarterenol). Colterol selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. This increases air flow and prevents bronchospasms and may eventually lead to an improvement of airway function.


Cartilage extracted from various parts of a cow and is proposed to stimulate the immune system and inhibit tumor cell growth. It was used in the 1950s and 60s to enhance wound healing. (NCI)


A member of the nerve growth factor family of trophic factors. In the brain BDNF has a trophic action on retinal, cholinergic, and dopaminergic neurons, and in the peripheral nervous system it acts on both motor and sensory neurons. (From Kendrew, The Encyclopedia of Molecular Biology, 1994)


The sodium salt form of bromfenac, a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and anti-inflammatory activities. Upon ophthalmic administration, bromfenac binds to and inhibits the activity of cyclooxygenase II (COX II), an enzyme which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins (PG). By inhibiting PG formation, bromfenac is able to inhibit PG-induced inflammation, thereby preventing vasodilation, leukocytosis, disruption of the blood-aqueous humor barrier, an increase in vascular permeability and an increase in intraocular pressure (IOP).


The nitrate salt form of butaconazole, a synthetic imidazole derivative with fungistatic properties. Butoconazole nitrate interferes with steroid biosynthesis by inhibiting the conversion of lanosterol to ergosterol, thereby changing the fungal cell membrane lipid composition. This alters cell permeability and leads to growth inhibition. Butaconazole nitrate is active against many dermatophytes and yeasts. It also contains antibacterial effects against some gram-positive organisms.


A synthetic ergoline derivative and a long-acting dopamine receptor agonist with high affinity for the dopamine D2 receptor. Cabergoline exerts an inhibitory effect on prolactin secretion by acting on dopamine receptors present in pituitary lactotrophs. This drug also binds to dopamine D2 receptors in the corpus striatum, thereby mimicking the actions of dopamine on motor control. Cabergoline also possesses antioxidant and neuroprotective properties due to its free radical scavenging activity. Cabergoline is used in the treatment of Parkinson's disease and in the treatment of hyperprolactinemia.


A colorless crystalline or white powdery organic, tricarboxylic acid occurring in plants, especially citrus fruits, and used as a flavoring agent, as an antioxidant in foods, and as a sequestrating agent. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)


An agent composed of urea and hydrogen peroxide. As an earwax removal agent, carbamide peroxide releases, upon administration into the ear, oxygen and causes foaming which helps soften, loosen and remove excessive earwax. It is also used as a disinfectant and in dentistry for its teeth whitening effects.


carbomer homopolymer type b (allyl sucrose crosslinked)


A third generation semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefpodoxime's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefpodoxime inhibits bacterial septum and cell wall synthesis formation.


The sodium salt form of ceftiofur, a semisynthetic, beta-lactamase-stable, broad-spectrum, third-generation cephalosporin with antibacterial activity. Ceftiofur binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.


A succinimide with anticonvulsant properties. Although the exact mechanism of action of methsuximide is unclear, it is thought to increase the seizure threshold and suppress the paroxysmal three-cycle-per-second spike-and-wave pattern seen with absence (petit mal) seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex and elevation of the threshold of the CNS to convulsive stimuli, probably due to direct modification of membrane function in excitable cells and/or alteration of chemically mediated neurotransmission.


The essential oil extracted from the flowers of Anthemis nobilis or Matricaria chamomilla. Chamomile oil is used in various preparations for calming and relaxing effects, especially on the nervous and digestive systems.


Aquaporin 1 forms a water-specific channel that is constitutively expressed at the PLASMA MEMBRANE of ERYTHROCYTES and KIDNEY TUBULES, PROXIMAL. It provides these cells with a high permeability to WATER. In humans polymorphisms of this protein result in the Colton blood group antigen.


The sodium succinate salt form of chloramphenicol, a nitrobenzene derivate and broad-spectrum antibiotic with antibacterial activity. Chloramphenicol sodium succinate reversibly binds to the 50S subunit of bacterial ribosomes, thereby interfering with peptidyl transferase activity in the elongation process of protein synthesis. As a result, this agent prevents bacterial cell growth.


An ester or salt of the bile acid cholic acid that is synthesized in the liver from cholesterol, with surfactant and signaling activities in the liver and intestine. In the intestine, cholate acts as a surfactant that promotes the absorption of dietary lipids and fat-soluble vitamins. In the liver, cholate's surfactant activity facilitates biliary excretion of xenobiotics and metal cations. Cholate binds to nuclear receptors, including farnesoid X receptor (FXR), pregnane X receptor (PXR), and the vitamin D receptor (VDR), which directly modulate gene transcription. Cholate may also be used as a biomarker for hepatotoxicity.


The sodium salt of colistimethate, a broad-spectrum polymyxin antibiotic against most aerobic Gram-negative bacteria except Proteus bacteria. Colistimethate sodium contains the pentasodium salt of the penta(methanesulfonic acid) derivative of colistin A as the major component and a small proportion of the petasodium salt of the pentamethanesulfonate derivative of colistin B. Colistins are cyclic polypeptides produced from Bacillus colistinus or B. polymyxa and function as a surfactant which penetrates into and disrupts the bacterial cell membrane, thereby resulting in bactericidal effect.


A sodium phosphate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones. (NCI04)


The maleate salt form of dexbrompheniramine, an alkylamine derivative with anticholinergic and sedative properties. Dexbrompheniramine is a histamine H1-receptor antagonist that competes with histamine for the H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract. The antagonistic action of this agent blocks the activities of endogenous histamine, which subsequently leads to temporary relief from the negative histamine-mediated symptoms of allergic reaction such as bronchoconstriction, vasodilation, increased capillary permeability and spasmodic contractions of gastrointestinal smooth muscle.


An imidazole derivate and active d-isomer of medetomidine with analgesic, anxiolytic and sedative properties. Dexmedetomidine selectively binds to presynaptic alpha-2 adrenoceptors located in the brain, thereby inhibiting the release of norepinephrine from synaptic vesicles. This leads to an inhibition of postsynaptic activation of adrenoceptors, which inhibit sympathetic activity, thereby leading to sedation and anxiolysis. The analgesic effect of this agent is mediated by binding to alpha-2 adrenoceptors in the spinal cord.


A sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.


A prazosin-related compound that is a selective alpha-1-adrenergic blocker.


The mineral component of bones and teeth; it has been used therapeutically as a prosthetic aid and in the prevention and treatment of osteoporosis.


A deoxythymidine analog with activity against herpes simplex virus. Edoxudine is activated by viral thymidine kinase to the 5'-monophosphate which is further phosphorylated by cellular enzymes to the 5'-triphosphate, a competitive inhibitor of the viral-coded DNA polymerase.


A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.


The hydrochloride salt form of esmolol, a short, rapid-acting, selective beta-adrenergic receptor blocker, devoid of intrinsic sympathomimetic activity, and with anti-arrhythmic, antihypertensive and potential analgesic activities. Upon intravenous administration, esmolol binds to and blocks the beta-1 receptor in the myocardium thereby preventing the action of epinephrine and norepinephrine. This leads to a reduction in the force and rate of cardiac contractions and thereby preventing tachycardia, arrythmias and/or hypertension. At higher doses, esmolol also blocks beta-2 receptors located in bronchial and vascular smooth muscle, thereby leading to smooth muscle relaxation. In addition, esmolol exerts a peripheral analgesic effect and intraoperative use of this agent may decrease the amount of opioid administration postoperatively. As the ester moiety in esmolol is rapidly hydrolyzed byplasma esterases, this agent has a very short half-life. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C72617" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C72617" NCI Thesaurus)


The citrate salt of a nonsteroidal triphenylethylene antiestrogen. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator (SERM). This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene also has intrinsic estrogenic properties, which is manifested depending on the tissue or species. (NCI04)


The propionate salt form of fluticasone, a synthetic trifluorinated glucocorticoid receptor agonist with antiallergic, antiinflammatory and antipruritic effects. Binding and activation of the glucocorticoid receptor results in the activation of lipocortin that in turn inhibits cytosolic phospholipase A2, which triggers cascade of reactions involved in synthesis of inflammatory mediators, such as prostaglandins and leukotrienes. Secondly, mitogen-activated protein kinase (MAPK) phosphatase 1 is induced, thereby leads to dephosphorylation and inactivation of Jun N-terminal kinase directly inhibiting c-Jun mediated transcription. Finally, transcriptional activity of nuclear factor (NF)-kappa-B is blocked, thereby inhibits the transcription of cyclooxygenase 2, which is essential for prostaglandin production.


A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.


A gadolinium chelate paramagnetic contrast agent. When placed in a magnetic field, gadoterate meglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI.


A semi-synthetic glycosaminoglycan (GAG) prepared by extracting GAGs from bovine tracheal cartilage and consisting of mostly chondroitin sulfate, with anti-arthritic activities in animals including dogs. Upon administration, polysulfated GAG (PSGAG), a proteolytic enzyme inhibitor, may inhibit various processes that lead to the loss of cartilaginous mucopolysaccharides. This may include the inhibition of interleukin-1 (IL-1)-mediated inflammation and degradation of cartilage proteoglycans and collagen. PSGAG may also stimulate the synthesis of protein, collagen, proteoglycans, and hyaluronic acid, which may improve joint function.


A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer.


A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.


The hydrochloride salt form of guanidine, a strong basic compound with parasympathomimetic activity. Guanidine hydrochloride enhances the release of acetylcholine following a nerve impulse and potentiates acetylcholine actions on muscarinic and nicotinic receptors. It also appears to slow the rates of depolarization and repolarization of muscle cell membranes. (NCI05)


A type of H. influenzae isolated most frequently from biotype I. Prior to vaccine availability, it was a leading cause of childhood meningitis.


A long-acting, synthetic nonapeptide analog of gonadotropin-releasing hormone (GnRH) with potential anti-tumor activity. Upon administration, histrelin binds to and activates GnRH receptors; prolonged administration results in pituitary GnRH receptor desensitization and inhibition of follicle stimulating hormone (FSH) and luteinizing hormone (LH) secretion, leading to a significant decline in testosterone production in males and may inhibit androgen receptor-positive tumor progression; in females, prolonged administration results in decreased estradiol production.


The fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outward potassium currents. This results in prolongation of atrial and ventricular action potential duration and refractory periods. Ibutilide slightly decreases the sinus rate and atrioventricular (AV) conduction and produces a dose-related prolongation of the QT interval. (NCI05)


A dibenzothiazepine derivative with antipsychotic property. Quetiapine fumarate antagonizes serotonin activity mediated by 5-HT 1A and 5-HT2 receptors. With a lower affinity, this agent also reversibly binds to dopamine D1 and D2 receptors in the mesolimbic and mesocortical areas of the brain leading to decreased psychotic effects, such as hallucinations and delusions. In addition, quetiapine also binds to other alpha-1, alpha-2 adrenergic and histamine H1 receptors.


A recombinant human insulin analog with rapid-acting, blood glucose-lowering activity. Insulin aspart, acting faster than regular human insulin, regulates glucose metabolism by binding to insulin receptors on muscle and fat cells, thereby facilitating the cellular uptake of glucose. This lowers blood glucose levels. At the same time, insulin aspart inhibits the liver's conversion of stored glycogen into glucose, which also contributes to lower blood glucose levels. Insulin aspart also inhibits lipolysis in adipose tissue, inhibits proteolysis, and enhances protein synthesis. (NCI05)


A heterodimeric cytokine that plays a role in innate and adaptive immune responses. Interleukin-12 is a 70 kDa protein that is composed of covalently linked 40 kDa and 35 kDa subunits. It is produced by DENDRITIC CELLS; MACROPHAGES and a variety of other immune cells and plays a role in the stimulation of INTERFERON-GAMMA production by T-LYMPHOCYTES and NATURAL KILLER CELLS.


A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.


An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE.


eighteen-carbon essential fatty acids that contain three double bonds; includes alpha linolenate, an omega-3 fatty acid, and gamma linolenate, an omega-6 fatty acid.


A polyunsaturated long-chain fatty acid with an 18-carbon backbone and exactly three double bonds. At least 17 different isomers of this compound are recognized.


A centrally acting muscle relaxant, chemically similar to amitriptyline hydrochloride with antidepressant activity. The exact mechanism of action of cyclobenzaprine hydrochloride has not been fully determined. However, it primarily acts at the brain stem to reduce tonic somatic motor activity, influencing both gamma and alpha motor neurons. This leads to a reduction in muscle spasms.


The citrate salt of lithium, a monovalent cation with antimanic activity. Although the exact mechanism is unclear, lithium might exert its mood-stabilizing effect via reduction of catecholamine concentration mediated through transneuronal membrane transport of sodium ion by sodium-potassium-stimulated adenosine triphosphatase (Na-K-ATPase). Alternatively, lithium may decrease cyclic adenosine monophosphate (cAMP) concentrations, which would desensitize hormonal-sensitive adenylyl cyclase receptors. Furthermore, lithium, in recommended dosage, blocks the activity of inositol-1-phosphatase, thereby resulting in the subsequent decrease of postsynaptic second messengers, diacylglycerol and inositol triphosphate, that contribute to chronic cell stimulation by altering electrical activity in the neuron.


A synthetic mast cell stabilizing compound with anti-inflammatory activity. Lodoxamide appears to inhibit the antigen-stimulated calcium transport across the mast cell membrane, thereby inhibiting mast cell degranulation and the release of histamine, leukotrienes, and other substances that cause hypersensitivity reactions. Lodoxamide also inhibits eosinophil chemotaxis. When applied topically to the eye, this drug prevents the symptoms associated with keratitis or conjunctivitis.


The olamine salt form of ciclopirox, a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. Ciclopirox exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).


An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.


The etabonate salt form of loteprednol, an ophthalmic analog of the corticosteroid prednisolone with anti-inflammatory activity. Loteprednol etabonate exerts its effect by interacting with specific intracellular receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Loteprednol etabonate specifically induces phospholipase A2 inhibitory proteins (collectively called lipocortins), which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes.


The citrate salt of the element magnesium with cathartic activity. The cathartic action of magnesium cations appears to result, in part, from osmotically mediated water retention, which subsequently stimulates peristalsis. In addition, magnesium ions may also stimulate the activity of nitric oxide (NO) synthase and increase the biosynthesis of the phospholipid proinflammatory mediator platelet activating factor (PAF) in the gut. NO may stimulate intestinal secretion via prostaglandin- and cyclic GMP-dependent mechanisms while PAF produces significant stimulation of colonic secretion and gastrointestinal motility.


An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed)


A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.


14 carbon straight chain saturated fatty acid common in membrane phospholipids and fatty acylated proteins.


A synthetic, aminoester, local, anesthetic agent. At the injection site, chloroprocaine hydrochloride acts by inhibiting sodium influx through binding to specific membrane sodium ion channels in the neuronal cell membranes, restricting sodium permeability, and blocking nerve impulse conduction. This leads to a loss of sensation. Chloroprocaine hydrochloride is short-acting due to rapid hydrolysis by pseudocholinesterase into para-aminobenzoic acid in plasma.


A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.


A nonsteroidal arylsulfonamide with anti-inflammatory properties. Nimesulide inhibits the cyclooxygenase-mediated conversion of arachidonic acid to pro-inflammatory prostaglandins. Modestly selective for COX-2, this agent binds to the enzyme, thereby inactivating it. Nimesulide may inhibit some carcinogenic COX-2-related carcinogenic effects on xenobiotic metabolism, apoptosis, immune surveillance and angiogenesis (overexpressed COX-2 in tumor epithelial cells enhances production of vascular growth factors and the formation of capillary-like networks). (NCI04)


nonionic surfactant with nine repeating ethoxy (oxy-1,2-ethanediyl) groups; a spermatocide, formulated primarily as a component of vaginal foams and creams.


FATTY ACIDS which have the first unsaturated bond in the sixth position from the omega carbon. A typical American diet tends to contain substantially more omega-6 than OMEGA-3 FATTY ACIDS.


The chloride salt form of oxybutynin, a tertiary amine and anticholinergic agent with antispasmodic activity. Oxybutynin chloride exerts its antimuscarinic effect on bladder smooth muscle by blocking muscarinic receptors in smooth muscle, thereby inhibiting acetylcholine binding. This results in a relaxation of bladder smooth muscle, a reduction of involuntary muscle contractions and delays the initial desire to void.


A mixture containing 2-amino-2-methyl-1-propanol and 8-bromotheophylline (a methylxanthine) in a 1:1 ratio, with mild diuretic activity.


An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.


An orally available bromide salt form of pinaverium, a calcium channel blocker (CCB) with antispasmodic activity. Upon oral administration, pinaverium blocks the voltage-dependent calcium channels and inhibits calcium ion influx into the smooth muscle cells located in the gastrointestinal (GI) tract. This prevents smooth muscle contraction and relaxes the GI tract. In addition, pinaverium may both reduce bowel uptake of and facilitate the function of locally active, co-administered drugs.


The maleate salt form of dexchlorpheniramine, an alkylamine, and first-generation histamine antagonist with anti-allergic activity. Dexchlorpheniramine maleate competitively blocks H1 receptors, thereby preventing the actions of histamine on bronchial smooth muscle, capillaries and gastrointestinal (GI) smooth muscle. This prevents histamine-induced bronchoconstriction, vasodilation, increased capillary permeability, and GI smooth muscle spasms.


A potassium salt used to replenish ELECTROLYTES, for restoration of WATER-ELECTROLYTE BALANCE, as well as a urinary and systemic alkalizer, which can be administered orally or by intravenous infusion. Formerly, it was used in DIURETICS and EXPECTORANTS.


A powder that dissolves in water, which is administered orally, and is used as a diuretic, expectorant, systemic alkalizer, and electrolyte replenisher.


A semi-synthetic beta-lactamase inhibitor isolated from streptomyces. Clavunalate potassium contains a beta-lactam ring and binds strongly to beta-lactamase at or near its active site. This protects other beta-lactam antibiotics from beta-lactamase catalysis. This drug is used in conjunction with beta-lactamase susceptible penicillins to treat infections caused by beta-lactamase producing organisms.


The dipotassium form of phosphoric acid, that can be used as an electrolyte replenisher and with radio-protective activity. Upon oral administration, potassium phosphate is able to block the uptake of the radioactive isotope phosphorus P 32 (P-32).


The sodium phosphate salt form of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. As a glucocorticoid receptor agonist, prednisolone sodium phosphate binds to specific intracellular glucocorticoid receptors, and causes the ligand- receptor complex to be translocated to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as various cytokines and lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both potent mediators of inflammation. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.


The sodium succinate salt form of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisolone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cells populations. (NCI)


The pamoate salt of pyrvinium, a quinoline-derived cyanine dye and an mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with anthelmintic and potential antineoplastic activities. Upon administration, pyrvinium pamoate may inhibit mitochondrial OxPhos and mitochondrial respiration, decreases mitochondrial function, prevents tumor cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell proliferation and leading to tumor cell death in some types of cancer cells. Mitochondrial OxPhos is overactivated in cancer cells and plays a key role in tumor cell proliferation. Drug resistant tumor cells are very susceptible to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease in mitochondrial function by increasing glycolysis.


A member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.


A broad-spectrum antibiotic that is being used as prophylaxis against disseminated Mycobacterium avium complex infection in HIV-positive patients.


Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION.


A derivative of prednisolone, a synthetic glucocorticoid with anti-inflammatory and immunosuppressive property. Upon binding to the cytosolic glucocorticoid receptor and cell entry, rimexolone activates specific glucocorticoid response elements, resulting in altered gene expression. These include induction of synthesis of anti-inflammatory protein IkappaB-alpha and inhibition of synthesis of nuclear factor kappaB (NFkappa B). As a result, pro-inflammatory cytokine production such as interleukin-1 (IL-1), IL-2 and IL-6 is down-regulated and cytotoxic T-lymphocyte activation inhibited. Therefore, an overall reduction in chronic inflammation and autoimmune reactions may be achieved.


Calcium Chloride 0.0014 MEQ/ML / K+ Chloride 0.004 MEQ/ML / NaCl 0.103 MEQ/ML / Sodium Lactate 0.028 MEQ/ML Injectable Solution

calcium chloride 0.0014 MEQ/ML / potassium chloride 0.004 MEQ/ML / sodium chloride 0.103 MEQ/ML / sodium lactate 0.028 MEQ/ML Injectable Solution

Calcium Chloride 0.0014 MEQ/ML / Pot Chloride 0.004 MEQ/ML / NaCl 0.103 MEQ/ML / Sodium Lactate 0.028 MEQ/ML Injectable Solution


A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION.


The bromide salt form of methscopolamine, a quaternary ammonium derivative of scopolamine with anticholinergic properties. Methscopolamine bromide exerts its effect on muscarine receptors in the gastrointestinal tract, thereby blocking the actions of acetylcholine. This leads to an inhibition of gastric secretions and gastrointestinal motility.


The biologically active fragment of human growth hormone-releasing factor, consisting of GHRH(1-29)-amide. This N-terminal sequence is identical in several mammalian species, such as human, pig, and cattle. It is used to diagnose or treat patients with GROWTH HORMONE deficiency.


The nitrate salt form of oxiconazole, a broad spectrum imidazole derivative with antifungal activity. Although the exact mechanism of action has yet to be fully elucidated, oxiconazole, like other azole antifungals, most likely inhibits the cytochrome P450-dependent demethylation of lanosterol. This prevents the synthesis of ergosterol which is a crucial component of fungal cell membrane. By disrupting fungal cell membrane synthesis and integrity, oxiconazole alters fungal cell membrane permeability, promotes loss of essential intracellular components and eventually inhibits fungal cell growth.


The hydrochloride salt form of sibutramine, a phenethylamine derivative with appetite depressant property. Sibutramine hydrochloride metabolites M1 and M2 competitively inhibit the reuptake of norepinephrine, serotonin, and to a lesser degree dopamine by pre-synaptic nerve terminals, thereby promoting a sense of satiety, leading to a decrease in calorie intake, and possibly an increase in resting metabolic rate. This agent does not exhibit anticholinergic or antihistaminic effects.


The trihydrate sodium salt of acetic acid, which is used as a source of sodium ions in solutions for dialysis and as a systemic and urinary alkalizer, diuretic, and expectorant.


The sodium salt form of alginic acid and gum mainly extracted from the cell walls of brown algae, with chelating activity. Upon oral administration, sodium alginate binds to and blocks the intestinal absorption of various radioactive isotopes, such as radium Ra 226 (Ra-226) and strontium Sr 90 (Sr-90).


The sodium salt of BENZOIC ACID. It is used as an antifungal preservative in pharmaceutical preparations and foods. It may also be used as a test for liver function.


The sodium salt of indanyl carbenicillin, a broad-spectrum, semi-synthetic carboxypenicillin antibiotic with bactericidal activity. Carbenicillin acylates C-terminal domain of penicillin-sensitive transpeptidase, resulting in opening the lactam ring of the antibiotic. This inactivation prevents the formation of the cross-linkage of peptidoglycan strands, thereby inhibiting the third and last stage of bacterial cell wall synthesis. As a result, cell wall integrity is compromised and cell lysis may follow. This agent is used mainly for gram-negative infections, and has limited gram-positive coverage.


A trihydroxy bile salt that is used as a digestive aid in dietary supplements. It is used in culture media and in conjunction with PAPAIN and PANCREATIN.


The sodium salt of citrate with alkalinizing activity. Upon absorption, sodium citrate dissociates into sodium cations and citrate anions; organic citrate ions are metabolized to bicarbonate ions, resulting in an increase in the plasma bicarbonate concentration, the buffering of excess hydrogen ion, the raising of blood pH, and potentially the reversal of acidosis. In addition, increases in free sodium load due to sodium citrate administration may increase intravascular blood volume, facilitating the excretion of bicarbonate compounds and an anti-urolithic effect.


The sodium salt of gluconic acid with chelating property. Sodium gluconate chelates and forms stable complexes with various ions, preventing them from engaging in chemical reactions.


The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.


The sodium salt form of phenylacetate with ammonia detoxifying activity. Upon administration, sodium phenylacetate binds to glutamine thereby forming phenylacetylglutamine and is thus excreted by the kidneys. By serving as an alternative to urea for the excretion of waste nitrogen, sodium phenylacetate is able to lower ammonia levels in the blood and prevent hyperammonemia.


A potassium ion exchange resin composed of benzene-diethyl polymer with ethenyl-benzene, sulfonated, sodium salt. Administered as an oral suspension, sodium polystyrene sulfonate lowers serum potassium levels by exchanging its sodium ions for potassium ions. Acting primarily in the large intestine, this agent also exchanges its sodium ions for calcium and magnesium ions, resulting in a decrease in serum calcium and magnesium levels. (NCI04)


The sodium salt form of propionic acid, a short chain fatty acid (SCFA) and food additive, with potential gastrointestinal (GI) protective activity. Upon oral administration of sodium propionate, it converts to propionic acid which may protect the GI tract and reduce incidence and severity of GI toxicity from radiation therapy.


The disodium salt of selenious acid. It is used therapeutically to supply the trace element selenium and is prepared by the reaction of SELENIUM DIOXIDE with SODIUM HYDROXIDE.


An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.


The nitrate salt form of sulconazole, a synthetic imidazole derivative with antifungal property. Sulconazole nitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and inhibition of the synthesis of ergosterol, an important component of the fungal cell membrane. Inhibition of ergosterol synthesis leads to a disruption of cell membrane permeability, and ultimately inhibition of cell wall synthesis. In addition, sulconazole nitrate seems to interfere with the autolytic degradation of fungal DNA and RNA.


A cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death.


A gamma-emitting RADIONUCLIDE IMAGING agent used in the evaluation of regional cerebral blood flow and in non-invasive dynamic biodistribution studies and MYOCARDIAL PERFUSION IMAGING. It has also been used to label leukocytes in the investigation of INFLAMMATORY BOWEL DISEASES.


Lipoglycopeptide antibiotic from Actinoplanes teichomyceticus active against gram-positive bacteria. It consists of five major components each with a different fatty acid moiety.


A broad spectrum antibiotic used as a second-line antitubercular drug, effective against pulmonary and extrapulmonary tuberculosis. Terizidone has activity against Mycobacterium strains that are resistant to first-line drugs.


A synthetic triglycyllysine derivative of vasopressin with vasoconstrictive, antihemorrhagic, and antidiuretic properties. Upon intravenous administration, terlipressin, an inactive prodrug, is biotransformed to its active moiety, lysine vasopressin (LVP), a nonselective vasopressin analogue with affinity for vasopressin receptors V1 (V1a), V2 and V3 (V1b). As a V1 agonist, terlipressin increases systemic vascular resistance, particularly in the splanchnic area, resulting in a decrease of portal pressure. V1 binding also promotes platelet aggregation and glycogenolysis, while V3 binding induces adrenocorticotropic hormone (ACTH) secretion. Compared to vasopressin, terlipressin has a minimal effect on V2 receptors, which are responsible for promotion of water reabsorption in the collecting ducts of the kidney via stimulation of cyclic AMP production.


The hydrochloride salt form of trimethobenzamide, a benzamide derivative with an antiemetic property. Although the mechanism of action is largely unknown, it inhibits the chemoreceptor trigger zone (CTZ), an area in the medulla oblongata through which emetic impulses are conveyed to the vomiting center, thereby suppressing nausea and vomiting.


An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.


The trisodium salt of a synthetic organic analogue of inorganic pyrophosphate with antiviral activity. Foscarnet selectively blocks the pyrophosphate binding site of herpesvirus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. This agent does not require phosphorylation by thymidine kinase (TK) or other kinases and therefore is active in vitro against herpes simplex virus (HSV) TK deficient mutants and cytomegalovirus (CMV) UL97 mutants. Because foscarnet crosses the blood brain barrier, it may be used in the treatment of viral infections of the CNS.


The hydrochloride salt form of pramoxine, a morpholine derivative with local anesthetic property. Pramocaine hydrochloride decreases the permeability of the neuronal membrane to sodium ions by reversibly binding to and inhibiting voltage-gated sodium channels. This results in stabilization of the membrane and, thereby inhibiting the ionic fluxes required for membrane depolarization, hence resulting in the failure to initiate a propagated action potential and subsequent conduction blockade.


An organic, iodinated radiopaque X-ray contrast medium used in diagnostic radiography. The iodine moiety of diatrizoate is not penetrable by X-rays, therefore it blocks the X-ray film exposure by radiation. This makes it possible to distinguish, on X-ray film, body parts that contain diatrizoate meglumine from body parts that do not contain this agent and allows for visualization of different body structures.


The hydrochloride salt form of tetrahydrozoline, an imidazole derivative with sympathomimetic property. Applied locally to the eye or nose, tetrahydrozoline binds to and activates alpha-adrenergic receptors, resulting in vasoconstriction and decreased nasal and ophthalmic congestion.


A phenylalkylamine sympathomimetic amine with appetite depressant property. Phendimetrazine tartrate is a prodrug that is hydrolyzed to the active metabolite phenmetrazine, which competes with norepinephrine and dopamine for their presynaptic transporters, thereby blocks the reuptake of these monoamines at the neuronal junctions. As a result, this prolongs activities of dopamine and norepinephrine and leads to central nervous system (CNS) stimulation and metabolic effects, including appetite-suppression, decreased gastric acid secretion and increased blood pressure.


A salt produced by the reaction of zinc oxide with acetic acid and used as an astringent, styptic, and emetic.


A nutritional supplement containing the zinc salt form of gluconic acid for the purpose of providing zinc. As an essential trace element, zinc is of key importance in many biological processes, acts as an antioxidant and strengthens the immune system. Although the mechanism of action is not completely known, zinc supplementation may be used to increase immunity against viruses or may interfere with the replication of certain viruses, such as the human papillomavirus (HPV).


A dietary zinc supplement containing the zinc salt of picolinic acid, that can be used to prevent or treat zinc deficiency, and with immunomodulatory activity. Upon administration, zinc picolinate supplements zinc. As an essential trace element, zinc is of key importance in many biological processes. It plays an important role in the proper functioning of the both the innate and adaptive immune system. Zinc inhibits the production of pro-inflammatory mediators and prevents inflammation. It acts as an antioxidant, prevents oxidative damage and protects cells against DNA damage. Zinc is required for the enzyme activities necessary for cell division, cell growth, and wound healing.


A species of nematodes in the family Ancylostomatidae. A. caninum infects domestic dogs and wild canids. It occasionally infects cats and humans. It is largely restricted to temperate, tropical, and sub-tropical regions.


A technetium imaging agent used to reveal blood-starved cardiac tissue during a heart attack.


The acetate salt form of sermorelin, a synthetic, amidated 29-amino acid peptide that corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone (GHRH). Sermorelin acetate directly stimulates the pituitary gland, resulting in release of growth hormone leading to increased plasma growth hormone, which is responsible for many biological processes and counteracts growth hormone deficiency.


Enzymes that catalyze the degradation of collagen by acting on the peptide bonds.


The citrate salt form of sufentanil, a synthetic congener of fentanyl and related to the phenylpieridines, with analgesic property. Sufentanil citrate binds to and activates the mu-opioid receptor, thereby producing analgesia, respiratory depression, miosis, reduced gastrointestinal motility, and euphoria. In addition, this agent has a more rapid onset of action and shorter duration of action compared to fentanyl.


A naturally occurring polysaccharide composed of beta-1,4-linked glucosamine residues with potential antineoplastic activity. Upon administration, poliglusam may, through a not yet fully elucidated mechanism, reduce advanced glycation end product (AGE) levels. This may reduce the interaction between AGEs and the receptor for advanced glycation end products (RAGE, AGER), which is overexpressed in some tumor types and is associated with poor patient outcomes. AGE-RAGE interaction may induce the phosphorylation and subsequent degradation of retinoblastoma protein (Rb), a key cell cycle inhibitor and tumor suppressor, through the phosphoinositide 3-kinase (PI3K)/protein kinase B (PKB, Akt) signaling pathway. Hyperphosphorylation of Rb leads to the dissociation of the Rb-E2F complex, which triggers the activation of genes required for G1/S transition and tumorigenesis. Reducing AGE levels may limit AGE-RAGE interaction and normalize the G1 to S-phase transition, potentially reducing the development and progression of certain cancers. AGEs are non-enzymatic protein modifications produced during the normal aging process that have been shown to play a role in the development and progression of some cancers.


An oxazolidinone with centrally-acting skeletal muscle relaxant properties. Although the exact mechanism through which metaxalone exerts its effect is largely unknown, it might be due to general central nervous system (CNS) depression. Metaxalone has no direct effect on the contractile mechanisms of striated muscle, the motor end plate, or the nerve fiber.


The oil extracted from the leaves of various Eucalyptus species. Eucalyptus oil is used for its aromatic properties and as an ingredient in pharmaceutical and industrial applications.


A phytonutrient and plant indole found in cruciferous vegetables including broccoli, Brussels sprouts, cabbage, cauliflower and kale, with potential anti-androgenic and antineoplastic activities. As a dimer of indole-3-carbinol, diindolylmethane (DIM) promotes beneficial estrogen metabolism in both sexes by reducing the levels of 16-hydroxy estrogen metabolites and increasing the formation of 2-hydroxy estrogen metabolites, resulting in increased antioxidant activity. Although this agent induces apoptosis in tumor cells in vitro, the exact mechanism by which DIM exhibits its antineoplastic activity in vivo is unknown.


A uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy. Overall, the gene expression changes associated with BVDU treatment result in the decrease or prevention of chemoresistance. In addition, this agent has been shown to enhance the cytolytic activity of NK-92 natural killer cells towards a pancreatic cancer cell line in vitro.


A macrocyclic lactone derived from Streptomyces cyanogriseus with antiparasitic activity. Upon administration, moxidectin may bind to glutamate-gated chloride channels (GluCl), gamma-aminobutyric acid (GABA) receptors and/or ATP-binding cassette (ABC) transporters expressed on nematode neurons and pharyngeal muscle cells. As a result, neurons or muscle cells remain at either hyperpolarization or depolarization state, thereby resulting in muscle paralysis. Moxidectin reduces the motility and fertility of the parasite and its excretion of immunomodulatory proteins, and inhibits the release of microfilariae.


Chromium Piccolinate is a salt of the trace metallic element chromium (Cr), essential in glucose metabolism. Found in vitamins and mineral supplements, Chromium may be necessary for utilization of dietary sugars and carbohydrates by optimizing the effects of insulin. Animal studies suggest that chromium picolinate may be carcinogenic, it enters cells directly and can causes mutations. (NCI04)


A piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.


A long-acting, quinazolinesulfonamide derivative with thiazide-like diuretic activity. Quinethazone acts in a similar manner to that of other typical thiazide diuretics and is no longer commercially available in the United States.


An analogue of consensus interferon which contains an additional methionyl amino acid residue. Consensus interferon (also known as interferon alfacon-1, rCon-IFN, and CIFN) is a genetically engineered synthetic interferon created from the most common amino acid sequences from the naturally occurring alpha interferons. Alpha interferons bind to specific cell-surface receptors, resulting in the transcription and translation of genes whose protein products have antiviral, antiproliferative, anticancer, and immune-modulating effects.


A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.


A synthetic acyclic guanine derivative with antiviral activity, mainly used to treat infections from herpes simplex virus (HSV) types 1 and 2. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding. As a result, herpes viral DNA synthesis and replication are selectively inhibited.


A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.


A non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Trandolaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Trandolaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


An inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis. (NCI04)


A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.


A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.


An angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, imidapril is converted by hydrolysis in the liver into its active form imidaprilat. Imidaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Imidaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.


A nitrocatechol compound with anti-parkinsonian property. Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT), which catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure including dihydroxyphenylalanine (DOPA), catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. When administered in conjunction with dopaminergic agents such as L-DOPA, entacapone prevents the metabolism and inactivation of adjunct drugs, thereby increasing the bioavailability of these compounds by facilitating their passage across the blood-brain barrier.


The sodium salt of risedronic acid, a synthetic pyridinyl bisphosphonate. Risedronic acid binds to hydroxyapatite crystals in bone and inhibits osteoclast-dependent bone resorption.


A 39 amino acid peptide and synthetic version of exendin-4, a hormone found in the saliva of the venomous lizard Gila monster, with insulin secretagogue and antihyperglycemic activity. Exenatide is administered subcutaneously and mimics human glucagon-like peptide-1 (GLP-1). Compared to GLP-1, exenatide has a longer half-life of 2.4 hours.


The synthetic benzoate ester of estradiol, a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. This agent exhibits mild anabolic and metabolic properties, and increases blood coagulability. (NCI04)


A 20 amino acid long synthetic peptide with thrombin-specific anticoagulant properties. Bivalirudin reversibly binds thrombin, free as well as clot bound, at the catalytic site and the anion-binding exosite, thereby preventing the formation and activation of fibrin, factor XIIIa, and other coagulation factors. This drug is primarily used during coronary angioplasty procedures, in combination with aspirin, in patients with unstable angina.


A morpholine derivative that is a selective and potent noradrenaline reuptake inhibitor; it is used in the treatment of DEPRESSIVE DISORDER.


A recombinant form of endogenous human growth hormone (GH), a polypeptide produced by the anterior lobe of the human pituitary gland. GH exhibits growth-promoting effects and metabolic effects on carbohydrate, fat, protein and bone metabolism. GH stimulates protein synthesis and the uptake of amino acids into cells, and induces lipolysis in adipose tissues. The secretion of GH increases with sexual maturation and then declines steadily.


A synthetic derivative of thienobenzodiazepine with antipsychotic, antinausea, and antiemetic activities. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotoninergic, dopaminergic, muscarinic M1-5, histamine H1, and alpha-1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. The antinausea and antiemetic effects of this agent appear to be due to the blockade of 5-HT2 and 5-HT3 receptors for serotonin. Although its exact mechanism of action in schizophrenia is unknown, it has been proposed that olanzapine's antipsychotic activity is mediated through antagonism to dopamine D2 receptors with rapid ligand-receptor dissociation kinetics that help to minimize extrapyramidal symptoms (EPS). Olanzapine may also stimulate appetite.


A synthetic catecholamine with positive chronotropic and inotropic properties, used in echocardiography and diagnostic coronary angiography. Arbutamine binds to and activates beta-1 adrenergic receptors in the myocardium, thereby increasing heart rate and increasing force of myocardial contraction. By exerting a chronotropic and inotropic effect, arbutamine mimics the cardiac stress caused by exercise that may prevent adequate tissue perfusion and oxygenation, and may provoke myocardial ischemia in patients with coronary artery disease.


The essential oil extracted from the leaves and stems of various Cymbopogon species. Citronella oil is used for its aromatic properties in parfumary, cosmetics, candles and soaps, and as an insect repellant.


An ester alkaloid derived from Rauwolfia canescens with antihypertensive activity. Deserpidine is a competitive inhibitor of the angiotensin converting enzyme (ACE). By competing with angiotensin I for ACE, deserpidine blocks the conversion of angiotensin I to angiotensin II, which is a potent vasoconstrictor. Reduced level of serum angiotensin II causes a decrease in blood pressure. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.


aliphatic four carbon acids or their salts, substituted in any position with amino groups.


polyunsaturated 20-carbon essential fatty acid found in animal fat or formed in biosynthesis from dietary linoleic acid; also, its salts, esters, or anions; precursor in the biosynthesis of leukotrienes, prostaglandins, and thromboxanes.


water soluble vitamin found in many plant and animal tissues; deficiency results in scurvy.


chelating agent that binds calcium and heavy metal ions; used as an anticoagulant for blood specimens and for treatment of lead poisoning and hypercalcemia.


A cofactor for 1-carbon transfer involved with DNA synthesis.


amino acid formed in the metabolism of L-glutamic acid; it is the major inhibitory neurotransmitter in the central nervous system, and is also found in some extraneural tissue including kidney and pancreatic islet cells.


poly(acetylglucosamine-glucuronic acid), a highly adhesive mucopolysaccharide found in the intercellular cementing substance of skin and other tissues.


metabolite of chenodeoxycholate; solubilizes cholesterol and is therefore used to remove cholesterol-containing biliary obstructions (cholestasis, cholesterol gallstones).


A solid composed of active and/or inert ingredient(s) in a soft, non-adhesive and absorbent piece of fabric or other material.


An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.


A subclass of smectite and a natural aluminomagnesium silicate clay, with potential protective effect for the digestive tract mucosa, and anti-inflammatory and anti-diarrheal activities. Although the exact mechanism of action has yet to be fully elucidated, upon administration, montmorillonite may adsorb bacteria, bacterial enterotoxins, viruses and other potentially diarrheagenic substances. It may also bind to mucin and modify mucus properties, thereby enhancing the mucus barrier function.


Dried aged bark of a buckthorn, Rhamnus purshiana, that contains the anthraquinone EMODIN and cascarosides. It is used as a laxative (CATHARTICS).


A concentrated mixture of anthranol glycosides from cascara sagrada (dried bark of Rhamnus p.) and used as a laxative in constipation and various medical conditions, stimulant laxative Casanthranol encourages bowel movements by acting on the intestinal wall to increase muscle contractions. (NCI04)


A species of enveloped and spherical viruses with a capsid with T=16 icosahedral symmetry and surrounded by amorphous tegument, in the Herpesviridae family and Cytomegalovirus genus. The genome is composed of monopartite, linear double-stranded DNA. Human herpesvirus 5 is found in humans and causes mononucleosis-like symptoms in healthy individuals and pneumonia, hepatitis, encephalitis, myelitis, colitis, retinitis, neuropathy, mucoepidermoid carcinoma as well as other malignancies in immunocompromised persons, organ transplant recipients and newborn infants. Human herpesvirus 5 is transmitted congenitally or via direct person-to-person contact.


A racemic mixture of d-epinephrine and l-epinephrine.


The meglumine salt form of ioxaglate, an organic iodine compound and a radiographic contrast medium. Ioxaglate meglumine blocks x-rays as they pass through the body, thereby allowing body structures not containing iodine to be visualized. The degree of opacity produced by ioxaglate meglumine is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of ioxaglate meglumine. (NCI05)


The sodium salt form of ioxaglate, an organic iodine compound and a radiographic contrast medium. Ioxaglate sodium blocks x-rays as they pass through the body, thereby allowing body structures not containing iodine to be visualized. The degree of opacity produced by ioxaglate sodium is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of ioxaglate sodium. (NCI05)


The sulfate salt form of paromomycin, a structural derivative of neomycin, an aminoglycoside antibiotic with amebicidal and bactericidal effects against predominantly aerobic gram-negative bacteria. Paromomycin binds specifically to the RNA oligonucleotide at the A site of bacterial 30S ribosomes, thereby causing misreading and premature termination of translation of mRNA and inhibition of protein synthesis followed by cell death.


The hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.


The hydrochloride salt of vancomycin, a branched tricyclic glycosylated peptide with bactericidal activity against most organisms and bacteriostatic effect on enterococci. At a site different from that of penicillins and cephalosporins, vancomycin binds tightly to the D-alanyl-D-alanine portion of cell wall precursors, thereby interfering with bacterial cell wall synthesis. This leads to activation of bacterial autolysins that destroy the cell wall by lysis. Vancomycin may also alter the permeability of bacterial cytoplasmic membranes and may selectively inhibit RNA synthesis.


An antibiotic mixture originally isolated from Streptomyces pristinaspiralis. It is a mixture of compounds from STREPTOGRAMIN GROUP A: pristinamycin IIA and IIB and from STREPTOGRAMIN GROUP B: pristinamycin IA, pristinamycin IB, pristinamycin IC.


A heparin fraction with a mean molecular weight of 4500 daltons. It is isolated from porcine mucosal heparin and used as an antithrombotic agent. (From Merck Index, 11th ed)


A species of ENTEROVIRUS which is the causal agent of POLIOMYELITIS in humans. Three serotypes (strains) exist. Transmission is by the fecal-oral route, pharyngeal secretions, or mechanical vector (flies). Vaccines with both inactivated and live attenuated virus have proven effective in immunizing against the infection.


Low-molecular-weight fragment of heparin, having a 4-enopyranosuronate sodium structure at the non-reducing end of the chain. It is prepared by depolymerization of the benzylic ester of porcine mucosal heparin. Therapeutically, it is used as an antithrombotic agent. (From Merck Index, 11th ed)


A low molecular weight, synthetic heparin. As an anticoagulant/antithrombotic agent, dalteparin binds to antithrombin and enhances the inhibition of Factor Xa. Compared to unfractionated heparins, the use of dalteparin is associated with lower incidences of osteoporosis and heparin-induced thrombocytopenia. (NCI04)


The succinate salt form of sumatriptan, a member of the triptan class of compounds with anti-migraine property. Sumatriptan succinate selectively binds to and activates serotonin 5-HT1 receptors. This results in constriction of meningeal, dural, cerebral or pial blood vessels via stimulation of the 5-HT1B receptors, thereby reducing the vascular pulsation and may provide relief in migraine headaches. Furthermore, agonistic action of this agent through presynaptic stimulation of 5-HT1D and/or 5-HT1F receptors prevents release of vasoactive and pro-inflammatory neuropeptide (calcitonin gene-related peptide), thereby may also relieve migraine headaches. In addition, central inhibition of pain transmission via the inhibition of trigeminal neurons in the brain stems and upper spinal cord mediated by 5-HT1B, 5-HT1D or 5-HT 1F receptors also aides in the alleviation of migraine pain.


The type species of SIMPLEXVIRUS causing most forms of non-genital herpes simplex in humans. Primary infection occurs mainly in infants and young children and then the virus becomes latent in the dorsal root ganglion. It then is periodically reactivated throughout life causing mostly benign conditions.


An oily resin extracted from several species of Commiphora trees. Myrrh oil is used for its aromatic properties and in various medicinal preparations for its antiseptic properties.


A cyclic cytidine.Cifostodine is formed during digestion of ribonucleic acid by ribonuclease.


A non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moexiprilat competitively inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the actions of the potent vasoconstrictor angiotensin II and leads to vasodilatation. This agent also prevents angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis.


An indole derivative and a potent serotonin 5-HT3 receptor antagonist with anti-emetic property. Dolasetron blocks the activity of serotonin released from the enterochromaffin cells of the small intestine by selectively inhibiting and inactivating 5-HT3 receptors located on the nerve terminals of the vagus nerve in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. This results in suppression of signalling to trigger chemo- and radiotherapy induced nausea and vomiting.


A synthetic cyclic octapeptide analogue of somatostatin. Lanreotide binds to somatostatin receptors (SSTR), specifically SSTR-2 and also to SSTR-5 with a lesser affinity. However, compare with octreotide, this agent is less potent in inhibiting the release of growth hormone from the pituitary gland. Furthermore, lanreotide has an acute effect on decreasing circulating total and free insulin-like growth factor 1 (IGF-I). This agent is usually given as a prolonged-release microparticle or Autogel formulation for the treatment of acromegaly and to relieve the symptoms of neuroendocrine tumors.


An aminopurine derivative and prodrug of penciclovir which is a competitive inhibitor of herpes simplex 2 DNA polymerase. It is used to treat HERPES SIMPLEX VIRUS INFECTION.


An androstanol non-depolarizing neuromuscular blocking agent. It has a mono-quaternary structure and is a weaker nicotinic antagonist than PANCURONIUM.


Cetrorelix is a synthetic decapeptide which is structurally related to gonadotrophin-releasing hormone (luteinising-hormone releasing hormone). It acts as an LHRH antagonist. (from ASTA Medica)


The morpholinoethyl ester of mycophenolic acid (MPA) with potent immunosuppressive properties. Mycophenolate stops T-cell and B-cell proliferation through selective inhibition of the de novo pathway of purine biosynthesis. In vivo, the active metabolite, MPA, reversibly inhibits inosine 5'-monophosphate dehydrogenase, an enzyme involved in the de novo synthesis of guanine nucleotides. MPA displays high lymphocyte specificity and cytotoxicity due to the higher dependence of activated lymphocytes on both salvage and de novo synthesis of guanine nucleotides relative to other cell types. (NCI04)


A gadolinium-based paramagnetic contrast agent. When placed in a magnetic field, gadobenate dimeglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI.


A reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.


A recombinant granulocyte colony-stimulating factor (G-CSF) that is used in the treatment and prevention of NEUTROPENIA, preparation and collection of blood progenitor cells, and for use in PERIPHERAL BLOOD STEM CELL TRANSPLANTATION.


A synthetic pyrimidine-based antifolate. Pemetrexed binds to and inhibits the enzyme thymidylate synthase (TS), which catalyses the methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) to 2'-deoxythymidine-5'-monophosphate (dTMP), an essential precursor in DNA synthesis.


A synthetic, nonopiod, twenty-five amino acid polybasic peptide analogue of an omega-conotoxin derived from the marine snail Conus magus with analgesic activity. Ziconotide appears to block neuronal N-type voltage-sensitive calcium channels (NCCB), inhibiting transmission from pain-sensing primary nociceptors. This agent may exhibit significant analgesic activity in refractory pain.


A purified, natural saponin isolated from the soapbark tree Quillaja saponaria Molina with potential immunoadjuvant activity. When co-administered with vaccine peptides, QS21 may increase total antitumoral vaccine-specific antibody responses and cytotoxic T-cell responses.


The oil extracted from the seeds of Borago officinalis. Borage oil has anti-inflammatory properties and is used in skincare preparations.


Essential oil extracted from MELALEUCA ALTERNIFOLIA (tea tree). It is used as a topical antimicrobial due to the presence of terpineol.


A recombinant therapeutic agent chemically identical to endogenous human GM-CSF except a leucine substitution in position 23. Binding to specific cell surface receptors, sargramostim modulates the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production and may reverse treatment-induced neutropenias. This agent also promotes antigen presentation, up-regulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function; it may also augment host antitumoral immunity.


A low molecular weight heparin (LMWH), obtained by controlled enzymatic depolymerization of heparin from porcine intestinal mucosa, with antithrombotic properties. Tinzaparin is a potent inhibitor of several activated coagulation factors, especially Factors Xa and IIa (thrombin); its primary activity is mediated through the plasma protease inhibitor antithrombin. In addition, this agent may inhibit angiogenesis through: 1) competitive binding of the heparin-binding sites on endothelial cells for the proangiogenic cytokines vascular endothelial growth factor (VEGF) and beta-fibroblast growth factor (beta-FGF) and 2) increasing the release of tissue factor pathway inhibitor (TFPI), a negative regulator of angiogenesis.


A sialic acid-analogue neuraminidase inhibitor with antiviral activity. Administered into the respiratory tract by aerosol inhalation, zanamivir selectively binds to and inhibits influenza A and B virus neuraminidase-mediated cleavage of sialic acid residues in host cell membrane-bound glycoprotein receptors for influenza viruses, preventing the release of progeny viruses from host cell surfaces and, so, further viral replication.


An orally active nonpeptide triazole-derived antagonist of angiotensin (AT) II with antihypertensive properties. Valsartan selectively and competitively blocks the binding of angiotensin II to the AT1 subtype receptor in vascular smooth muscle and the adrenal gland, preventing AT II-mediated vasoconstriction, aldosterone synthesis and secretion, and renal reabsorption of sodium, and resulting in vasodilation, increased excretion of sodium and water, a reduction in plasma volume, and a reduction in blood pressure.


A lung surfactant agent that is used as a replacement for endogenous lung surfactant. Colfosceril palmitate is effective in reducing the surface tension of pulmonary fluids, thereby increasing lung compliance properties to prevent alveolar collapse and improve breathing. This drug is used in the treatment of neonatal respiratory distress.


A recombinant form of human granulocyte macrophage colony stimulating factor (GM-CSF), with potential immunostimulating activity. Upon administration as inhalation solution via nebulizer, molgramostim binds to specific cell surface receptors and promotes or restores GM-CSF signaling, thereby modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. This agent also activates neutrophils, monocytes, macrophages, and dendritic cells and promotes antigen presentation, upregulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin (IL)-2-mediated, lymphokine-activated killer cell function. In addition, the restoration of GM-CSF signaling promotes surfactant clearing by pulmonary alveolar macrophages.


A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.


A recombinant analog of the endogenous cytokine interleukin-2 (IL-2) with immunoregulatory and antineoplastic activities. Aldesleukin binds to and activates the IL-2 receptor, followed by heterodimerization of the cytoplasmic domains of the IL-2R beta and gamma(c) chains; activation of the tyrosine kinase Jak3; and phosphorylation of tyrosine residues on the IL-2R beta chain, resulting in an activated receptor complex. Various cytoplasmic signaling molecules are recruited to the activated receptor complex and become substrates for regulatory enzymes that are associated with the receptor complex. This agent enhances lymphocyte mitogenesis; stimulates long-term growth of human IL-2 dependent cell lines; enhances lymphocyte cytotoxicity; induces lymphokine-activated killer (LAK) cell and natural killer (NK) cell activities; and induces expression of interferon-gamma. Aldesleukin may induce T cell-mediated tumor regression in some tumor types.


A carbazole derivative and a selective serotonin receptor antagonist with antiemetic activity. Palonosetron competitively blocks the action of serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors located on vagal afferents in the chemoreceptor trigger zone (CTZ), resulting in suppression of chemotherapy-induced nausea and vomiting. The CTZ is located in the area postrema on the dorsal surface of the medulla oblongata at the caudal end of the fourth ventricle and outside the blood-brain barrier (BBB).


Six clades of the virus exist. But all are considered one species, since serotyping is not yet possible and they do not contain any other taxonomic characteristics except geographic distribution (8th ICTV Report).


OH- anion, found in common basic reagents and in biological ion transport and pH gradient systems.


four carbon intermediate metabolite, between fumarate and oxaloacetate, in the Krebs cycle.


An aromatic fatty acid metabolite of phenylalanine with potential antineoplastic activity. Naturally occurring in mammals, phenylacetate induces differentiation, growth inhibition, and apoptosis in tumor cells. Implicated mechanisms of action include decreased protein prenylation, activation of the peroxisome proliferation-activated receptors, inhibition of DNA methylation, and depletion of glutamine. (NCI04)


The hydrochloride salt form of apomorphine, a derivative of morphine and non-ergoline dopamine agonist with high selectivity for dopamine D2, D3, D4 and D5 receptors. Apomorphine hydrochloride acts by stimulating dopamine receptors in the nigrostriatal system, hypothalamus, limbic system, pituitary gland, and blood vessels. This enhances motor function, suppresses prolactin release, and causes vasodilation and behavioral effects. Apomorphine hydrochloride is used in the treatment of Parkinson's disease and erectile dysfunction. In addition, apomorphine hydrochloride acts on the chemoreceptor trigger zone and is used as a central emetic in the treatment of drug overdose.


The sodium salt form of phenytoin, a hydantoin derivate and non-sedative antiepileptic agent with anticonvulsant activity. Phenytoin sodium promotes sodium efflux from neurons located in the motor cortex, thereby stabilizing the neuron and inhibiting synaptic transmission. This leads to a reduction in posttetanic potentiation at synapses, an inhibition of repetitive firing of action potentials and ultimately inhibits the spread of seizure activity.


A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.


The hydrochloride salt form of flurazepam, a member of the benzodiazepines and a long-acting depressor of the central nervous system (CNS) with sedative and hypnotic effects. Flurazepam binds to a specific site on the benzodiazepine-gamma-aminobutyric acid (GABA)-A-chloride ionophore receptor complex located on the neuronal membrane. Binding causes an allosteric modification of the receptor thereby enhancing the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events, which leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential, and a decrease in neuronal excitability. By modulating binding of the GABA inhibitory neurotransmitter to GABA-A receptors in the ascending reticular activating system, flurazepam blocks arousal of the cortical and limbic system, thereby exerting its sedative and hypnotic effect.


The hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen.


The hydrochloride salt form of the d-isomer of synthetic diphenyl propionate derivative propoxyphene, with narcotic analgesic effect. This agent mimics the effects of the endogenous opiate dextropropoxyphene, by binding to mu receptors located throughout the central nervous system. The binding results in GTP to GDP exchanges on the mu-G-protein complex, by which effector adenylate cyclase is inactivated thereby decreasing intracellular cAMP. This, in turn, inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, dextropropoxyphene closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels. This results in hyperpolarization, thereby reducing neuronal excitability, which further decreases the perception of pain.


The maleate salt form of triethylperazine, a piperazine phenothiazine derivative and a dopamine antagonist used as antiemetic. Thiethylperazine blocks postsynaptic dopamine 2 (D2) receptors in the medullary chemoreceptor trigger zone (CTZ), thereby decreasing stimulation of the vomiting center in the brain. Peripherally, thiethylperazine blocks the vagus nerve in the gastrointestinal tract. In addition, this agent also shows antagonistic activities mediated through muscarinic receptors, H1-receptors, and alpha(1)-receptors.


The maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property. Trimipramine maleate appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action.


A synthetic, intermediate-acting mono-quaternary steroid and non-depolarizing neuromuscular blocking agent, with muscle relaxant activity. Vecuronium competitively binds to and blocks the nicotinic acetylcholine receptor at the neuromuscular junction, thereby preventing acetylcholine (ACh) binding and resulting in skeletal muscle relaxation and paralysis. Vecuronium has a shorter duration of action than pancuronium.


A species of gram-negative bacteria that is the etiologic agent of bacillary angiomatosis (ANGIOMATOSIS, BACILLARY). This organism can also be a cause of CAT-SCRATCH DISEASE in immunocompetent patients.


A yellowish fossil resin, the gum of several species of coniferous trees, found in the alluvial deposits of northeastern Germany. It is used in molecular biology in the analysis of organic matter fossilized in amber.


A gray substance found in the GASTROINTESTINAL TRACT of the SPERM WHALE.


A species of gram-negative, anaerobic, rod-shaped bacteria originally classified within the BACTEROIDES genus. This bacterium is a common commensal in the gingival crevice and is often isolated from cases of gingivitis and other purulent lesions related to the mouth.


The sodium salt of docusate, a dioctyl salt and an emollient laxative with stool-softening activity. Docusate decreases surface tension and emulsification of fecal matter and allows water to penetrate and mix with stool. As a result, it softens the stool.


A phenolic phytochemical naturally occurring in extra virgin olive oil, with potential antioxidant, anti-inflammatory and cancer preventive activities. Although the mechanisms of action through which hydroxytyrosol exerts its effects have yet to be fully determined, this agent affects the expression of various components of the inflammatory response, possibly through the modulation of the nuclear factor-kappa B (NF-kB) pathway. The effects include the modulation of pro-inflammatory cytokines, such as the inhibition of interleukin-1alpha (IL-1a), IL-1beta, IL-6, IL-12, and tumor necrosis factor-alpha (TNF-a); increased secretion of the anti-inflammatory cytokine IL-10; inhibition of the production of certain chemokines, such as C-X-C motif chemokine ligand 10 (CXCL10/IP-10), C-C motif chemokine ligand 2 (CCL2/MCP-1), and macrophage inflammatory protein-1beta (CCL4/MIP-1b); and inhibition of the expression of the enzymes inducible nitric oxide synthase (iNOS/NOS2) and prostaglandin E2 synthase (PGES), which prevent the production of nitric oxide (NO) and prostaglandin E (PGE2), respectively. In addition, hydroxytyrosol is able to regulate the expression of other genes involved in the regulation of tumor cell proliferation, such as extracellular signal-regulated and cyclin-dependent kinases. Also, hydroxytyrosol scavenges free radicals and prevents oxidative DNA damage. This induces apoptosis and inhibits proliferation in susceptible cancer cells.


A 2-oxo monocarboxylic acid anion that is the conjugate base of pyruvic acid, which is an important metabolic product for energy-producing biochemical pathways. Pyruvate is the final product of glycolysis and, when hypoxic conditions arise, can be metabolized anaerobically to form lactate. This chemical is a precursor of both acetyl-coenzyme A and oxaloacetate, which are involved in the citric acid cycle. Additionally, oxaloacetate is a substrate in the gluconeogenesis pathway.


A selective benzothiophene estrogen receptor modulator (SERM). Raloxifene binds to estrogen receptors (ER) as a mixed estrogen agonist/antagonist; it displays both an ER-alpha-selective partial agonist/antagonist effect and a pure ER-beta-selective antagonist effect. This agent functions as an estrogen agonist in some tissues (bones, lipid metabolism) and as an estrogen antagonist in others (endometrium and breasts), with the potential for producing some of estrogen's beneficial effects without producing its adverse effects. (NCI04)


A water-soluble phosphate ester prodrug of phenytoin, a hydantoin derivative with anticonvulsant activity. Fosphenytoin is hydrolyzed to phenytoin by phosphatases. Phenytoin exerts its effect mainly by promoting sodium efflux and stabilizes neuronal membranes in the motor cortex. This leads to a suppression of excessive neuronal firing and limits the spread of seizure activity.


The amino acid analog fluorodopa (FDOPA) labeled with fluorine F 18, a positron-emitting isotope, with potential tumor tracer property. Fluorine F 18 fluorodopa is able to cross the blood-brain barrier and is taken up by brain tumor cells. As uptake is higher in tumor cells, tumors may then be imaged using positron emission tomography (PET). Assessing tumor uptake of FDOPA may be beneficial for diagnosis, localization and in determining further treatment.