Aono M, Moriga M, Mizuta K, Narusawa H
Gastroenterol Jpn. 1986 Jun;21(3):213-9. doi: 10.1007/BF02774563.
The effects of histamine H2-receptor antagonists on acetylcholinesterase and pseudocholinesterase activity were studied. All H2-antagonists tested inhibited both enzyme activities dose-dependently. The potency of inhibitory activity of H2-antagonists on acetylcholinesterase estimated from median inhibitory dose were in the following order of decreasing activity: ranitidine greater than TZU-0460 greater than cimetidine greater than YM-11170, whereas that on pseudocholinesterase were TZU-0460 greater than ranitidine greater than cimetidine greater than YM-11170. As the effects derived from the inhibition of acetylcholinesterase by H2-antagonists may affect intestinal motility, we studied ileal muscle contractions. Ranitidine had the most potent stimulating effect on contraction, the pattern of which was similar to physostigmine and was blocked by atropine and morphine. YM-11170 had a weak action on muscle contraction and cholinesterase activities.
研究了组胺H2受体拮抗剂对乙酰胆碱酯酶和假性胆碱酯酶活性的影响。所有测试的H2拮抗剂均剂量依赖性地抑制这两种酶的活性。根据半数抑制剂量估算，H2拮抗剂对乙酰胆碱酯酶的抑制活性强度按活性递减顺序排列为：雷尼替丁＞TZU - 0460＞西咪替丁＞YM - 11170，而对假性胆碱酯酶的抑制活性强度为：TZU - 0460＞雷尼替丁＞西咪替丁＞YM - 11170。由于H2拮抗剂抑制乙酰胆碱酯酶所产生的效应可能会影响肠道蠕动，因此我们研究了回肠肌肉收缩情况。雷尼替丁对收缩具有最强的刺激作用，其收缩模式类似于毒扁豆碱，且可被阿托品和吗啡阻断。YM - 11170对肌肉收缩和胆碱酯酶活性的作用较弱。
