大鼠尾动脉交感神经末梢毒蕈碱受体亚型的鉴定

Characterization of the muscarine receptor subtype on sympathetic nerve endings in the rat caudal artery.

作者信息

Shen A, Mitchelson F

机构信息

School of Pharmacology, Victorian College of Pharmacy (Monash University), Parkville, Australia.

出版信息

Eur J Pharmacol. 1994 Feb 3;252(2):167-72. doi: 10.1016/0014-2999(94)90593-2.

DOI:10.1016/0014-2999(94)90593-2

PMID:7512503

Abstract

The prejunctional muscarine receptor on sympathetic nerves in the rat caudal artery was characterized using several selective antagonists. The inhibitory response of carbachol on vasoconstriction elicited by sympathetic nerve stimulation was antagonized by benzhexol (trihexyphenidyl; pKB 7.1), heptane-1,7-bis(dimethyl-3'-phthalimidopropyl ammonium bromide) (C7/3-phth; pKB 6.5) and hexahydrosiladifenidol (HHSiD; apparent pKB 6.0). These pKB values suggest that the receptor most closely resembles the muscarine M2 receptor subtype rather than the muscarine M1, M3 or M4 receptor subtypes.

摘要

运用多种选择性拮抗剂对大鼠尾动脉交感神经上的节前毒蕈碱受体进行了特性鉴定。苯海索（安坦；pKB 7.1）、庚烷-1,7-双（二甲基-3'-邻苯二甲酰亚胺丙基溴化铵）（C7/3-邻苯二甲酰亚胺；pKB 6.5）和六氢硅二苯哌啶（HHSiD；表观pKB 6.0）可拮抗卡巴胆碱对交感神经刺激所引发的血管收缩的抑制反应。这些pKB值表明，该受体与毒蕈碱M2受体亚型最为相似，而非毒蕈碱M1、M3或M4受体亚型。