新型毒蕈碱受体激动剂AF102B的交感兴奋作用及其被哌仑西平阻断的情况。

Sympathoexcitatory action of a novel muscarinic receptor agonist, AF102B, and its blockade by pirenzepine.

作者信息

Yoshioka M, Togashi H, Matsumoto M, Morii K, Saito H

机构信息

First Department of Pharmacology, Hokkaido University School of Medicine, Sapporo, Japan.

出版信息

Pharmacol Toxicol. 1990 Jul;67(1):84-7. doi: 10.1111/j.1600-0773.1990.tb00788.x.

DOI:10.1111/j.1600-0773.1990.tb00788.x

PMID:2395822

Abstract

The pharmacological effects of a novel, selective muscarinic (M1) receptor agonist, AF102B (cis-2-methyl-spiro-(1,3-oxathiolane-5,3')-quinuclidine hydrochloride hemihydrate), on sympathetic nerve activity are described. Intravenous administration of AF102B (1 and 10 mg/kg) produced a dose-dependent increase in cardiac sympathetic nerve activity accompanied by tachycardia in spinal-intact rats. In addition, AF102B (10 mg/kg) caused a marked increase in cardiac sympathetic nerve activity and heart rate in pithed rats. Pirenzepine (50 micrograms/kg) inhibited these sympathoexcitatory effects of AF102B (10 mg/kg) in pithed rats. These findings suggest that AF102B possesses a sympathoexcitatory action which is mediated by M1-receptors.

摘要

本文描述了一种新型选择性毒蕈碱（M1）受体激动剂AF102B（顺式-2-甲基-螺-(1,3-氧硫杂环戊烷-5,3')-奎宁环盐酸盐半水合物）对交感神经活动的药理作用。静脉注射AF102B（1和10毫克/千克）可使脊髓完整的大鼠心脏交感神经活动呈剂量依赖性增加，并伴有心动过速。此外，AF102B（10毫克/千克）可使去大脑大鼠的心脏交感神经活动和心率显著增加。哌仑西平（50微克/千克）可抑制AF102B（10毫克/千克）对去大脑大鼠的这些交感兴奋作用。这些发现表明，AF102B具有由M1受体介导的交感兴奋作用。