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CAS NO.773092-05-0
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773092-05-0 for sale trader oxytocin Good Supplier In China
In June 2013, the Ministry of Health, Labor and Welfare in Japan approved acotiamide (also referred to as Z-338 and YM443), for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia (FD). Acotiamide enhances acetylcholine release from enteric neurons through selective muscarinic acetylcholine receptor M1, M2 antagonism, and inhibition of AChE, thereby enhancing gastric emptying and gastric accommodation. Acotiamide inhibits the acetylcholine-induced Ca2+-activated Cl-current with an IC50 of 1.8 μM in oocytes expressing muscarinic M1 receptors and in oocytes expressing muscarinic M2 receptors, acotiamide inhibited the acetylcholine-induced K+ currents with an IC50 of 10.1 μM. However, studies in conscious dogs, guinea-pig gastric muscle strips and assays with human cholinesterase indicate that acotiamide inhibits AChE with a Ki of 610 nM suggesting that acotiamide stimulates gastric motility mainly by inhibiting AChE activation. In a restraint stress-induced rat model, acotiamide significantly improved delayed gastric emptying and feeding inhibition but did not affect normal gastric emptying or feeding in intact rats. A synthetic route to acotiamide that employs pyridine hydrochloride to selectively cleave a 2-substituted methyl ether from a 2,4,5-trimethoxy benzamide intermediate, as a key step, has been reported.
Acotiamide, also known as YM-443 and Z-338, is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia. It acts as an acetylcholinesterase inhibitor. Note: The Approved drug API is a cotiamide HCl trihydrate
Acotiamide, also known as YM-443 and Z-338, is a drug approved in Japan for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia.
atalogue Number | A190240 |
Chemical Name | Acofide Trihydrate |
Synonyms | Acotiamide Hydrochloride Trihydrate; N-(2-(Diisopropylamino)ethyl)-2-(2-hydroxy-4,5-dimethoxybenzamido)thiazole-4-carboxamide Hydrochloride Trihydrate. |
CAS Number | 773092-05-0 |
Alternate CAS # | Free form (185106-16-5) |
Molecular Formula | C??H??N?O?S • (HCl) • 3(H ?O) |
Appearance | Pale Yellow Solid |
Melting Point | 193-195o C |
Molecular Weight | 450.55 + 36.46 + 3(18.02) |
Storage | Hygroscopic, -20°C Freezer, Under inert atmosphere |
Solubility | Chloroform (Slightly, Heated, Sonicated), DMSO (Slightly) Methanol (Slightly) |
Category | Standards; Pharmaceutical/API Drug Impurities/Metabolites; |
Applications | Acofide Trihydrate is a gastrointestinal prokinectic agent used in the treatment of functional malnutrition. A tablet for the treatment of functional dyspepsia. |