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[青蛙(林蛙)和太平洋褶柔鱼胆碱能受体及胆碱酯酶特性的比较]

[Comparison of the cholinoreceptor and cholinesterase properties of the frog Rana temporaria and the squid Todarodes pacificus].

作者信息

Danilov A F, Viniar T N, Lavrent'eva V V, Rozengart E V

出版信息

Zh Evol Biokhim Fiziol. 1985 Mar-Apr;21(2):139-43.

PMID:3158137
Abstract

Studies have been made on the interaction of several groups of quartenary ammonium salts with cholinoreceptors of m. rectus abdominis of the frog Rana temporaria, and isolated m. retractor infundibuli of the octopus Todarodes pacificus, as well as with cholinesterases of the frog brain and visual ganglia of the octopus. The derivatives of polymethylene bis(trimethylammonium) compounds, being cholinomimetic drugs for frog muscle, do not exert cholinomimetic influence on octopus muscle. The same difference with respect to their effect on frog and octopus receptors was found in anabazin derivatives. Among amide derivatives of acetylcholine, the strongest mimetic effect on cholinoreceptors of both animals was exhibited by a piperazine isolog with gauche-conformation, whereas N-methyl isolog with trans-conformation was found to be the strongest inhibitor of cholinesterases. Cholinoreceptors and cholinesterase of the octopus were less sensitive to the effect of the investigated quartenary ammonium salts than those of the frog.

摘要

已经对几组季铵盐与泽蛙腹直肌、太平洋褶柔鱼的漏斗缩肌以及蛙脑和太平洋褶柔鱼视觉神经节的胆碱酯酶之间的相互作用进行了研究。聚亚甲基双(三甲基铵)化合物的衍生物作为蛙肌肉的拟胆碱药物,对章鱼肌肉没有拟胆碱作用。在杀鼠灵衍生物中也发现了它们对蛙和章鱼受体作用的相同差异。在乙酰胆碱的酰胺衍生物中,具有gauche-构象的哌嗪类似物对两种动物的胆碱受体表现出最强的模拟作用,而具有反式构象的N-甲基类似物被发现是胆碱酯酶的最强抑制剂。章鱼的胆碱受体和胆碱酯酶对所研究的季铵盐的作用比蛙的更不敏感。

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