Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.

 Nizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. [1] Nizatidine also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. [2]

 Nizatidine exhibits maximal inhibition of gastric acid in rats within the first hour of drug administration, with EC50 of 1.383 μmol/kg. [1] Nizatidine (0.3-3 mg/kg, i.v.) significantly increases the motor index of gastrointestinal (GI) motility in a dose-dependent manner. Nizatidine inhibits gastric acid secretion with ED50 and ED90 of 0.18 and 3.22 mg/kg in dogs, and 2.94 and 19.6 mg/kg in rats, respectively. [2]

 

References

[1] Lin TM, et al. J Pharmacol Exp Ther, 1986, 239(2), 406-410.

[2] Ueki S, et al. J Pharmacol Exp Ther, 1993, 264(1), 152-157.

http://www.selleck.cn/products/Cimetidine(Tagamet).html

转载本文请联系原作者获取授权，同时请注明本文来自陈达科学网博客。
链接地址：https://wap.sciencenet.cn/blog-2321593-935924.html

上一篇：RO4929097 is a γ secretase inhibitor
下一篇：Cimetidine, a histamine congener, competitively inhibits