豚鼠输精管中组胺能受体的鉴定及特异性阻断

Identification and specific blockade of histaminergic receptors in guinea pig vasa deferentia.

作者信息

Joshi D P, Verma S C

出版信息

Can J Physiol Pharmacol. 1981 Oct;59(10):1089-93. doi: 10.1139/y81-166.

PMID:6119147

Abstract

Histamine produces contractions of the guinea pig vas deferens. The present investigation was undertaken to characterize the nature of histaminergic receptors in this tissue. Histamine (1.6 X 10(-6) M to 3.2 X 10(-5) M) produced dose-related contractions of guinea pig vas deferens (GPVD). Mepyramine (5.3 X 10(-8) M and 1 X 10(-9) M) blocked the responses to histamine competitively. Metiamide (1.23 X 10(-5) M) did not block the responses to histamine significantly. Specific H1 and H2 receptor agonists, namely 2-(2'-pyridyl)ethylamine (PEA) (2.55 X 10(-6) M to 3.0 X 10(-5) M) and 4-methylhistamine (4-MH) (2.52 X 10(-5) M to 3.0 X 10(-4) M), respectively, produced dose-related contractions of GPVD. The responses to PEA were blocked competitively by mepyramine, whereas the responses to 4-MH were blocked by metiamide. Reserpine pretreatment (5 mg/kg, i.p., 24 h) did not alter the responses to histamine and PEA. Our data suggest the presence of both H1 and H2 receptors in the GPVD which are excitatory in nature.

摘要

组胺可使豚鼠输精管收缩。本研究旨在确定该组织中组胺能受体的性质。组胺（1.6×10⁻⁶M至3.2×10⁻⁵M）可使豚鼠输精管（GPVD）产生剂量相关的收缩。甲氧苄胺（5.3×10⁻⁸M和1×10⁻⁹M）竞争性阻断对组胺的反应。甲硫咪胺（1.23×10⁻⁵M）对组胺反应的阻断作用不显著。特异性H1和H2受体激动剂，即2-(2'-吡啶基)乙胺（PEA）（2.55×10⁻⁶M至3.0×10⁻⁵M）和4-甲基组胺（4-MH）（2.52×10⁻⁵M至3.0×10⁻⁴M），分别使GPVD产生剂量相关的收缩。对PEA的反应被甲氧苄胺竞争性阻断，而对4-MH的反应被甲硫咪胺阻断。利血平预处理（5mg/kg，腹腔注射，24小时）不改变对组胺和PEA 的反应。我们的数据表明，GPVD中同时存在H1和H2受体，其性质为兴奋性。