HETEROGENEITY OF HISTAMINE H1-RECEPTORS - SPECIES VARIATIONS IN [MEPYRAMINE-H-3 BINDING OF BRAIN MEMBRANES

被引：235

作者：

CHANG, RSL

TRAN, VT

SNYDER, SH

机构：

[1] JOHNS HOPKINS UNIV,SCH MED,DEPT PHARMACOL,BALTIMORE,MD 21205

[2] JOHNS HOPKINS UNIV,SCH MED,DEPT EXPTL THERAPEUT,BALTIMORE,MD 21205

[3] JOHNS HOPKINS UNIV,SCH MED,DEPT PSYCHIAT,BALTIMORE,MD 21205

[4] JOHNS HOPKINS UNIV,DEPT BEHAV SCI,BALTIMORE,MD 21205

来源：

JOURNAL OF NEUROCHEMISTRY | 1979年 / 32卷 / 06期

关键词：

D O I：

10.1111/j.1471-4159.1979.tb02276.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

[3H]Mepyramine binds with high affinity to membranes from brain of human, rat, guinea‐pig, rabbit and mouse with drug specificity indicating an association with histamine H1receptors. Considerable species differences occur in the affinity of [3H]mepyramine, with guinea‐pig and human having 34 times greater affinity than rat, mouse or rabbit. The greater affinity of [3H]mepyramine in guinea‐pig than in rat is attributable both to faster association and slower dissociation rates in guinea‐pig. Species differences in affinity for H1 receptor sites occur for some antihistamines but not for others. Some tricyclic antidepressant and neuroleptic drugs are extremely potent inhibitors of [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined. The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding. The regional distribution of specific [3H]mepyramine binding differs considerably in the various species examined. Copyright © 1979, Wiley Blackwell. All rights reserved

引用

页码：1653 / 1663

页数：11

共 30 条

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