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Restrict the search for
telotristat ethyl
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Class (Stereo):
CHEMICAL (ACHIRAL)
Cloxacepride is an amide of the dopamine antagonist metoclopramide. It was discovered in the 1980s by Merkle and Panlabs and was found to possess anti-allergic properties. Cloxacepride demonstrated activity in a rat Passive Cutaneous Anaphylaxis (PCA) model after oral administration. Cloxacepride did not protect against histamine-induced anaphylaxis in guinea pigs, thus it was concluded that the effect of cloxacepride is not mediated by histamine receptors. In experiments with human mast cells from adenoidal tissues, cloxacepride at concentrations 10-100 uM significantly inhibited concanavalin A (con A) induced histamine release. At higher concentrations, cloxacepride caused the release of histamine. These findings indicate that cloxacepride acts through calmodulin antagonism.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Alitame [l-α-aspartyl-N-(2,2,4,4-tetramethyl-3-thioethanyl)-d-alaninamide] is an amino acid-based sweetener developed by Pfizer Central Research from l-aspartic acid, d-alanine, and 2,2,4,4-tetraethylthioethanyl amine. A terminal amide group instead of the methyl ester constituent of aspartame was used to improve the hydrolytic stability. The incorporation of d-alanine as a second amino acid in place of l-phenylalanine has resulted in optimum sweetness. The increased steric and lipophilic bulk on a small ring with a sulfur derivative has provided a very sweet product and good taste qualities. Alitame is noncariogenic. From an oral intake, 7–22% is unabsorbed and excreted in the feces. The remainder is hydrolyzed to aspartic acid and alanine amide. The aspartic acid is normally metabolized, and the alanine amide is excreted in the urine as a sulfoxide isomer, sulfone, or conjugated with glucuronic acid. U.S. Food and Drug Administration has approved alitame for use as per acceptable daily intake (ADI) value.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Stilonium Iodide (also known as MG 624) is a trimethylethanaminium derivative with ganglionic-blocking action. Stilonium Iodide acts as α7-nicotinic receptor antagonist and Stilonium Iodide inhibits transmission between preganglionic and postganglionic neurons in the Autonomic Nervous System. Stilonium Iodide inhibits nicotine-induced proliferation and angiogenesis in human microvascular endothelial cells of the lung. Stilonium Iodide displayed anti-angiogenic activity in Matrigel, rat aortic ring and rat retinal explant assays. Furthermore, MG624 suppressed angiogenesis of NCI-H69 human SCLC tumors in vivo in both the chicken chorioallantoic membrane (CAM) and nude mice model.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Suxethonium is a depolarising muscle relaxant, with low incidence of postoperative muscle pain.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Sepazonium was studied as a topical anti-infective drug. However, information about the current use of this agent is not available.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Deditonium is an antibacterial compound developed by the French company Centre de Recherches des Laboratoires Diamant. Deditonium is a quaternary ammonium derivative and has a bacteriostatic action at concentrations ranging from 1x10-6 to 5x10-4 M. Gram-positive cocci were found to be the most sensitive as well as many enterobacteria.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Apadoline [RP 60180, RP 60180A, RPR 60180] is a κ-opioid receptor agonist which was undergoing phase II clinical trials with Aventis Pharma for the treatment of pain.
Class (Stereo):
CHEMICAL (RACEMIC)
Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.
Status:
Investigational
Source:
NCT01313572: Phase 3 Interventional Terminated Coronary Artery Disease
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Apadenoson (BMS-068645) is a selective adenosine 2A agonist that contains a methyl ester group which undergoes esterase hydrolysis to its acid metabolite. Apadenoson had been in phase III clinical trials by Forest (now a part of Allergan) for the treatment of coronary artery disease. However, this study has been terminated.
Status:
Investigational
Source:
USAN:ISOMYLAMINE HYDROCHLORIDE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
ISOMYLAMINE is a spasmolytic and smooth muscle relaxant.
