文章基本信息

标题：Depolarizing Neuromuscular Blocking Action of Coryneine Derived from Aconite Root in Isolated Mouse Phrenic Nerve-Diaphragm Muscles
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作者：Masayasu KIMURA ; Ikuko KIMURA ; Masashi MUROI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1995
卷号：18
期号：5
页码：691-695
DOI：10.1248/bpb.18.691
出版社：The Pharmaceutical Society of Japan
摘要：The mode of the neuromuscular blocking action of coryneine (a quaternary ammonium derivative of dopamine) derived from aconite root was investigated in isolated phrenic nerve-diaphragm muscles and denervated diaphragm muscles of mice. Coryneine (20-150μM) blocked the nerve-evoked twitch response without affecting the contraction evoked by electrical stimulation of the muscle. The blocking effect was reversed by neostigmine, a cholinesterase inhibitor. The electrical charge-response curve on depolarization produced by iontophoretically applied acetylcholine (ACh) at the endplate regions in normal muscles was shifted to the right on decreasing the maximal response by 40μM coryneine. The double-reciprocal plot revealed that coryneine reduced the apparent affinity of ACh for its receptor on decreasing the maximal response. Coryneine (20μM-2mM) itself depolarized the endplate membrane and this effect was reversibly suppressed by 1 and 5μM pancuronium. Coryneine (30μM-10mM) produced contractions of denervated muscles in a concentration-dependent manner and the effects were reduced by 70nM pancuronium. These results indicate that coryneine is a depolarizing agent and a mixed-type competitive and noncompetitive neuromuscular blocker.
关键词：coryneine;depolarizing neuromuscular block;phrenic nerve-diaphragm muscle