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Acotiamide Hydrochloride Hydrate

ACOTIAMIDE HYDROCHLORIDE HYDRATE

 

General Information:

Acotiamide HydrochlorideHydrate,aprokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.

Therapeutic Category:

Acotiamide HydrochlorideHydrate falls under the Gastrointestinal Agent.

 

Primary Characterstics:

IUPAC Name:

N-[2-[di(propan-2-yl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide;trihydrate;hydrochloride

Molecular Formula:
C21H37ClN4O8S

Molecular Weight:

541.1 g/mol

Molecular Structure:


 

 

Mechanism of Action:

·        Acotiamide Hydrochloride Hydrate, an AChE inhibitor, enhanced acetylcholine (ACh)-induced contraction and motility of the gastric antrum and body.

·        Acotiamide Hydrochloride Hydrate inhibited human AChE with mixed pattern (Ki1 = 0.61 ± 0.03 µM, Ki2 = 2.7 ± 0.2 µM, and IC50 = 3 µM) and suppressed the degradation of ACh released from cholinergic nerve terminals.

·        The AChE inhibitory effect of acotiamide almost disappeared by dialysis, which was shown to be reversible.

·        AcotiamideHydrochloride Hydrate did not show a high affinity to the muscarinic M1, M2, M3, dopamine D2S and serotonin 5-HT4 receptors involving in the regulation of gastrointestinal motility.