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乙哌立松在离体犬心房中的抗烟碱样和抗毒蕈碱样作用。

Anti-nicotinic and anti-muscarinic actions of eperisone in the isolated canine atrium.

作者信息

Saegusa K, Furukawa Y, Akahane K, Haniuda M, Chiba S

机构信息

Department of Pharmacology, Shinshu University School of Medicine, Matsumoto, Japan.

出版信息

Jpn J Pharmacol. 1991 Jun;56(2):187-93. doi: 10.1254/jjp.56.187.

Abstract

The effects of eperisone, an antispastic agent, on the chronotropic and inotropic responses to acetylcholine, nicotine or stimulation of intracardiac autonomic nerves were evaluated in isolated, blood-perfused canine atrium. Eperisone (10-300 micrograms) injected into the sinus node artery of the isolated atrium produced dose-related negative chronotropic and inotropic effects, which were not affected by atropine. In the same doses, eperisone inhibited the negative chronotropic and inotropic responses to an injection of acetylcholine and intracardiac parasympathetic stimulation. Eperisone also suppressed the negative followed by positive cardiac responses to nicotine, but did not modify the positive responses to intracardiac sympathetic stimulation or norepinephrine. The inhibitory effect persisted much longer for the responses to nicotine or parasympathetic stimulation than for those to acetylcholine. These results suggest that eperisone at doses that induce direct cardiac depressant effects exerts its blocking action on nicotinic receptors at parasympathetic ganglia and sympathetic nerve terminals and on muscarinic receptors at the effector cells in the dog heart.

摘要

在离体、血液灌注的犬心房中,评估了抗痉挛药物乙哌立松对乙酰胆碱、尼古丁或心内自主神经刺激所引起的变时性和变力性反应的影响。将乙哌立松(10 - 300微克)注入离体心房的窦房结动脉,可产生剂量相关的负性变时性和变力性作用,且不受阿托品影响。相同剂量下,乙哌立松可抑制注射乙酰胆碱和心内副交感神经刺激所引起的负性变时性和变力性反应。乙哌立松还可抑制对尼古丁的负性心脏反应,随后出现正性反应,但不改变对心内交感神经刺激或去甲肾上腺素的正性反应。对尼古丁或副交感神经刺激反应的抑制作用持续时间比对乙酰胆碱反应的抑制作用长得多。这些结果表明,在诱导直接心脏抑制作用的剂量下,乙哌立松对犬心脏副交感神经节和交感神经末梢的烟碱受体以及效应细胞的毒蕈碱受体发挥阻断作用。

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