Acotiamide HCl

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Chemical Structure| 185104-11-4 同义名 : Z-338; YM443; Acotiamide hydrochloride
CAS号 : 185104-11-4
货号 : A111223
分子式 : C21H31ClN4O5S
纯度 : 98%
分子量 : 487.013
MDL号 : MFCD23103502
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Acotiamide HCl, an oral first-in-class prokinetic drug. The drug modulates upper gastrointestinal motility to alleviate abdominal symptoms resulting from hypomotility and delayed gastric emptying. It exerts its activity in the stomach via muscarinic receptor inhibition, resulting in enhanced acetylcholine release and inhibition of acetylcholinesterase activity[1]. Acotiamide enhances the effect of acetylcholine in the enteric nervous system, enhances gastric contractility, and accelerates delayed gastric emptying. Acotiamide prolongs gastric accommodation and improves stress-induced impaired gastric accommodation[2]. Adding acotiamide to gastric acid inhibitors can improve symptoms in patients with refractory NERD (non-erosive reflux disease) [3]. Acotiamide is associated with lower antral pressures after nutrient intake, whereas it has no effect on fundic pressures, GE (gastric emptying) rate and symptom perceptions in HVs[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.27mL

2.05mL

1.03mL

20.53mL

4.11mL

2.05mL

参考文献

[1]Nowlan ML, Scott LJ. Acotiamide: first global approval [published correction appears in Drugs. 2014 Jun;74(9):1059. Nolan, Mary L [corrected to Nowlan, Mary L]]. Drugs. 2013;73(12):1377-1383

[2]Ikeo K, Oshima T, Sei H, et al. Acotiamide improves stress-induced impaired gastric accommodation. Neurogastroenterol Motil. 2017;29(4):10.1111/nmo.12991

[3]Mikami H, Ishimura N, Okada M, et al. Acotiamide Has No Effects on Esophageal Motor Activity or Esophagogastric Junction Compliance. J Neurogastroenterol Motil. 2018;24(2):241-247

[4]Masuy I, Tack J, Verbeke K, Carbone F. Acotiamide affects antral motility, but has no effect on fundic motility, gastric emptying or symptom perception in healthy participants. Neurogastroenterol Motil. 2019;31(4):e13540