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西咪替丁对麻醉猫的神经节阻断活性。

Ganglion blocking activity of cimetidine in the anaesthetized cat.

作者信息

Gwee M C, Cheah L S, Lee H S

出版信息

Clin Exp Pharmacol Physiol. 1985 Sep-Oct;12(5):475-80. doi: 10.1111/j.1440-1681.1985.tb00897.x.

Abstract

Cimetidine produced a dose-dependent and reversible inhibition of contractions of the nictitating membrane elicited through stimulation of the preganglionic nerve supplying the superior cervical ganglion in the anaesthetized cat. Postganglionic nerve stimulation resulted in only a slight and variable inhibition of the contractions. Both hexamethonium and cimetidine also produced a dose-dependent and reversible fall in arterial blood pressure. The ganglion blocking activity of cimetidine was much weaker than that of hexamethonium; the ED50 ratio (cimetidine:hexamethonium) calculated from the cumulative log dose-response curves for the two drugs was 64. The possible mechanism(s) of ganglion blockade produced by cimetidine is discussed including a possible action at nicotinic receptors, either directly or indirectly (via its anticholinesterase activity), and ion channel blockade. The clinical implications of cimetidine-induced ganglionic blockade are also discussed, especially with respect to sexual impotence associated with the use of cimetidine.

摘要

西咪替丁对麻醉猫颈上神经节节前神经刺激所引起的瞬膜收缩产生剂量依赖性且可逆的抑制作用。节后神经刺激仅导致收缩有轻微且可变的抑制。六甲铵和西咪替丁还会引起动脉血压剂量依赖性且可逆的下降。西咪替丁的神经节阻断活性比六甲铵弱得多;根据两种药物的累积对数剂量 - 反应曲线计算出的ED50比值(西咪替丁:六甲铵)为64。文中讨论了西咪替丁产生神经节阻断的可能机制,包括对烟碱受体可能直接或间接(通过其抗胆碱酯酶活性)的作用以及离子通道阻断。还讨论了西咪替丁诱导的神经节阻断的临床意义,特别是与使用西咪替丁相关的阳痿问题。

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