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大鼠离体尾动脉突触后α-肾上腺素能受体的特性研究

Characterization of postsynaptic alpha-adrenoceptors in the isolated rat tail artery.

作者信息

Savino E A, Varela A

机构信息

Cátedra de Fisiologia, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Argentina.

出版信息

Arch Int Pharmacodyn Ther. 1991 Jan-Feb;309:137-46.

PMID:1679620
Abstract

The main purpose was to assess the existence of alpha 2-adrenoceptors in isolated segments of the proximal portion of the rat tail artery. Adrenaline and phenylephrine evoked strong contractile responses, whereas in 22 out of 49 arteries, 10-100 microM clonidine evoked weak contractions. Guanabenz, idazoxan and yohimbine lacked contractile effects. Reserpine pretreatment did not modify the percentage of responsive arteries to clonidine nor the ineffectiveness of guanabenz. Raising the Ca2+ concentration to 2.5 mM did not alter the responsiveness to adrenaline and phenylephrine but enhanced the amplitude of the responses to clonidine. The exposure to 0.1 or 1.0 microM angiotensin did not affect the responsiveness to clonidine. Responses to clonidine were abolished by 10 nM prazosin and not affected by 1 microM idazoxan or yohimbine. Adrenaline and phenylephrine concentration-response curves were shifted rightward by prazosin and phentolamine (pA2 within 7.3-9.0) and by clonidine, guanabenz, idazoxan and yohimbine (pA2 lower than 6.5). These data suggest that the tail artery lacks postsynaptic alpha 2-adrenoceptors, that clonidine exerts partial alpha 1-agonist/antagonist effects and that guanabenz, idazoxan and yohimbine act as partial alpha 1-antagonists.

摘要

主要目的是评估大鼠尾动脉近端离体节段中α2-肾上腺素能受体的存在情况。肾上腺素和去氧肾上腺素可引起强烈的收缩反应,而在49条动脉中的22条,10 - 100微摩尔可乐定引起微弱收缩。胍那苄、咪唑克生和育亨宾无收缩作用。利血平预处理既未改变对可乐定反应的动脉百分比,也未改变胍那苄的无效性。将Ca2+浓度提高到2.5毫摩尔/升不会改变对肾上腺素和去氧肾上腺素的反应性,但会增强对可乐定反应的幅度。暴露于0.1或1.0微摩尔血管紧张素不会影响对可乐定的反应性。对可乐定的反应被10纳摩尔哌唑嗪消除,且不受1微摩尔咪唑克生或育亨宾影响。肾上腺素和去氧肾上腺素的浓度-反应曲线被哌唑嗪和酚妥拉明(pA2在7.3 - 9.0之间)以及可乐定、胍那苄、咪唑克生和育亨宾(pA2低于6.5)右移。这些数据表明尾动脉缺乏突触后α2-肾上腺素能受体,可乐定发挥部分α1-激动剂/拮抗剂作用,且胍那苄、咪唑克生和育亨宾作为部分α1-拮抗剂起作用。

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