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[使用烷化剂对骨骼肌胆碱能受体的研究]

[Study of skeletal muscle cholinoreceptors using alkylating agents].

作者信息

Shelkovnikov S A, Mikhel'son M Ia, Smirnova T S, Galakhova I E, Ioffe D V

出版信息

Farmakol Toksikol. 1979 Jan-Feb;42(1):19-23.

PMID:421885
Abstract

The ability of decamethonium containing beta-clorethylamino groups to alkylate the nicotinic cholinoreceptors of the frog tonic muscles was studied. D-tubocurarine prevented the action of the alkylating decamethonium (AD). The latter equally inhibited the effects of carbacholine and tetramethylammonium. The degree of alkylation did not change with pH varying from 6 to 11. AD did not produce any parallel shifts, but inhibited at once the maximal response to carbacholine both of the frog intact muscle and of a single tonic fibre. It is suggested that decamethonium blocks the cholinoreceptors anionic sites, which are represented by the carboxylate, or phosphate anions. The frog tonic muscle probably fails to posses any spare receptors.

摘要

研究了含β-氯乙氨基的十烃季铵使青蛙强直性肌烟碱型胆碱能受体烷基化的能力。筒箭毒碱可阻止烷基化十烃季铵(AD)的作用。后者同样抑制氨甲酰胆碱和四甲铵的效应。烷基化程度在pH值从6变化到11时不变。AD不会产生任何平行移位,但能立即抑制青蛙完整肌肉和单根强直性纤维对氨甲酰胆碱的最大反应。提示十烃季铵阻断了由羧酸盐或磷酸盐阴离子所代表的胆碱能受体阴离子位点。青蛙强直性肌可能没有任何备用受体。

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