蝗虫神经元章鱼胺受体的高亲和力拮抗剂。

High-affinity antagonists of the locust neuronal octopamine receptor.

作者信息

Roeder T

机构信息

Universität Hamburg, Zoologisches Institut, F.R.G.

出版信息

Eur J Pharmacol. 1990 Nov 27;191(2):221-4. doi: 10.1016/0014-2999(90)94151-m.

DOI:10.1016/0014-2999(90)94151-m

PMID:2086239

Abstract

The pharmacological antagonistic properties of the invertebrate specific octopamine receptor were investigated using a conventional radio-receptor assay with [3H]octopamine as the radioligand. Among the antagonists with highest affinity of the locust (Locusta migratoria L.) neuronal octopamine receptor were tetracyclic substances like mianserin (K1 = 1.2 nM), some of its derivatives (8-hydroxymianserin; K1 = 1.68 nM), and maroxepine, which is the antagonist with the highest affinity ever reported (K1 = 1.02 nM) to this octopamine receptor class. Among the other antagonists tested only phentolamine (K1 = 19 nM) and promethazine (K1 = 31.2 nM) had high-affinity properties.

摘要

使用以[3H]章鱼胺作为放射性配体的传统放射受体分析法，研究了无脊椎动物特异性章鱼胺受体的药理学拮抗特性。在对蝗虫（飞蝗）神经元章鱼胺受体具有最高亲和力的拮抗剂中，有四环类物质，如米安色林（K1 = 1.2 nM）、其一些衍生物（8-羟基米安色林；K1 = 1.68 nM）以及马罗塞平，马罗塞平是有史以来报道的对该类章鱼胺受体亲和力最高的拮抗剂（K1 = 1.02 nM）。在测试的其他拮抗剂中，只有酚妥拉明（K1 = 19 nM）和异丙嗪（K1 = 31.2 nM）具有高亲和力特性。