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Acotiamide hydrochloride

Names

[ CAS No. ]:
185104-11-4

[ Name ]:
Acotiamide hydrochloride

[Synonym ]:
N-[2-(Diisopropylamino)ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-1,3-thiazole-4-carboxamide hydrochloride (1:1)
Acotiamide hydrochloride
UNII:510791NN30
Z338
YM 443
4-Thiazolecarboxamide, N-[2-[bis(1-methylethyl)amino]ethyl]-2-[(2-hydroxy-4,5-dimethoxybenzoyl)amino]-, hydrochloride (1:1)

Biological Activity

[Description]:

Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].

[Related Catalog]:

Research Areas >> Others
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease
Signaling Pathways >> Neuronal Signaling >> AChE

[Target]

IC50: 1.79 μM (AChE)


[In Vitro]

Acotiamide hydrochloride (10, 30, 100 μM; 1 hour) reduces expression levels of IκB-α phosphorylation in LPS- and MCP-1-stimulated macrophage cell lines[1]. Cell Viability Assay[1] Cell Line: NR8383, macrophage Concentration: 10, 30, 100 μM Incubation Time: 1 hour Result: Significantly reduced both TNF-α and IL-6 productions in LPS/MCP-1-stimulated NR8383 cells.

[In Vivo]

Acotiamide hydrochloride (0.3, 1, 3 mg/kg; i.v./3, 10, 30 mg/kg; p.o.) increases the postprandial gastric motility index in a dose-dependent manner[2]. Acotiamide hydrochloride (0.83 mg/kg; i.v.; once) inhibits AChE in rat stomach with IC50 of 1.79 μM[3]. Animal Model: Male mongrel dogs (9-11 kg), Male beagle dogs (9.6-12.9 kg)[2] Dosage: 0.3, 1, 3, 10, 30 mg/kg Administration: Intravenous injection; once. Result: Increased the postprandial gastric motility. Animal Model: Male Sprague-Dawley rats (aged 6-7 weeks)[3]. Dosage: 0.83 mg/kg Administration: Intravenous injection; once. Result: Effectively improved functional dyspepsia by inhibiting AChE in rat stomach.

[References]

[1]. Kazuyoshi Y oshii, et al. Physiologically-Based Pharmacokinetic and Pharmacodynamic Modeling for the Inhibition of Acetylcholinesterase by Acotiamide, A Novel Gastroprokinetic Agent for the Treatment of Functional Dyspepsia, in Rat Stomach. Pharmaceutical Research, 33(2), 292–300.

[2]. Hiroshi Yamawaki, et al. Acotiamide attenuates central urocortin 2-induced intestinal inflammatory responses, and urocortin 2 treatment reduces TNF-α productions in LPS-stimulated macrophage cell lines. Neurogastroenterol Motil. 2020 Aug;32(8):e13813.

[3]. Matsunaga Y, Acotiamide hydrochloride (Z-338), a new selective acetylcholinesterase inhibitor, enhances gastric motility without prolonging QT interval in dogs: comparison with cisapride, itopride, and mosapride. J Pharmacol Exp Ther. 2011 Mar;336(3):791-800.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H31ClN4O5S

[ Molecular Weight ]:
487.013

[ Exact Mass ]:
486.170380

[ PSA ]:
148.24000

[ LogP ]:
4.72760

Related Compounds