豚鼠十二指肠中突触前α2-肾上腺素能受体亚型功能基础的测定

Determination on functional basis of presynaptic alpha 2-adrenoceptor subtypes in guinea-pig duodenum.

作者信息

Colucci R, Blandizzi C, Carignani D, Lazzeri G, Natale G, Crema F, Del Tacca M

机构信息

Institute of Pharmacology, School of Medicine and Dentistry, University of Pisa, Italy.

出版信息

Neurosci Lett. 1996 May 24;210(1):29-32. doi: 10.1016/0304-3940(96)12648-3.

DOI:10.1016/0304-3940(96)12648-3

PMID:8762184

Abstract

The effects of several alpha 2-adrenoceptor agonists and antagonists were examined on the cholinergic twitch contractions evoked by electrical field stimulation of guinea-pig duodenum. Oxymetazoline, xylazine, noradrenaline, alpha-methyl-noradrenaline or medetomidine (0.01-30 microM) were nearly equieffective in inhibiting duodenal twitch responses. The effects of xylazine were competitively counteracted by antagonists tested (0.03-10 microM) with the following order of potency: RX 821002 = idazoxan > rauwolscine = yohimbine = BRL 44408 >> prazosin = ARC 239 = BRL 41992. According to the current classification, it is suggested that alpha 2-heteroadrenoceptors involved in the modulation of duodenal cholinergic neurotransmission belong to the alpha ZD subtype.

摘要

研究了几种α2 -肾上腺素能受体激动剂和拮抗剂对豚鼠十二指肠电场刺激诱发的胆碱能抽搐收缩的影响。羟甲唑啉、赛拉嗪、去甲肾上腺素、α-甲基去甲肾上腺素或美托咪定（0.01 - 30微摩尔）在抑制十二指肠抽搐反应方面几乎具有同等效力。赛拉嗪的作用被所测试的拮抗剂（0.03 - 10微摩尔）竞争性拮抗，其效力顺序如下：RX 821002 = 咪唑克生 > 育亨宾碱 = 育亨宾 = BRL 44408 >> 哌唑嗪 = ARC 239 = BRL 41992。根据目前的分类，提示参与十二指肠胆碱能神经传递调节的α2 -异肾上腺素能受体属于αZD亚型。