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9-氨基-1,2,3,4-四氢吖啶(THA),一种据称可用于治疗阿尔茨海默病的药物,可抑制乙酰胆碱酯酶活性并减慢外向钾电流。

9-Amino-1,2,3,4-tetrahydroacridine (THA), an alleged drug for the treatment of Alzheimer's disease, inhibits acetylcholinesterase activity and slow outward K+ current.

作者信息

Drukarch B, Kits K S, Van der Meer E G, Lodder J C, Stoof J C

机构信息

Department of Neurology, Medical Faculty, Free University, Amsterdam, The Netherlands.

出版信息

Eur J Pharmacol. 1987 Sep 2;141(1):153-7. doi: 10.1016/0014-2999(87)90424-9.

Abstract

The in vitro release of acetylcholine in rat brain tissue was inhibited by 9-amino-1,2,3,4-tetrahydroacridine (THA). Atropine antagonized this effect of THA. As THA does not display an affinity for muscarinic receptors, we conclude that THA inhibits acetylcholinesterase activity. In electrophysiological studies with neurons of Lymnaea stagnalis, THA inhibited the slow outward K+ current and consequently increased the duration of the action potentials. It is discussed that both effects of THA possibly contribute to its reported effect in the treatment of patients with Alzheimer's disease.

摘要

9-氨基-1,2,3,4-四氢吖啶(THA)抑制大鼠脑组织中乙酰胆碱的体外释放。阿托品可拮抗THA的这一作用。由于THA对毒蕈碱受体没有亲和力,我们得出结论,THA抑制乙酰胆碱酯酶活性。在对椎实螺神经元的电生理研究中,THA抑制了缓慢的外向钾电流,从而延长了动作电位的持续时间。讨论了THA的这两种作用可能都有助于其在阿尔茨海默病患者治疗中所报道的效果。

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