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大鼠肛门尾骨肌和输精管后接头α-肾上腺素能受体的药理学分析。

Pharmacological analysis of the postjunctional alpha-adrenoceptors of the rat anococcygeus muscle and vas deferens.

作者信息

Adenekan O O, Tayo F M

出版信息

Arch Int Pharmacodyn Ther. 1985 Jul;276(1):106-11.

PMID:2996453
Abstract

The alpha-adrenoceptor sub-type of the rat vas deferens was characterized with noradrenaline (alpha-1, alpha-2-agonist), phenylephrine (alpha-1-agonist), prazosin (alpha-1-antagonist) and yohimbine (alpha-2-antagonist) and compared with the results obtained in the rat anococcygeus muscle. In the vas deferens, both prazosin and phentolamine were competitive antagonists of noradrenaline and phenylephrine whereas yohimbine was a non-competitive antagonist irrespective of the concentrations of these antagonists. On the other hand, in the anococcygeus muscle, at low concentrations, prazosin was non-competitive against noradrenaline whilst it was competitive against phenylephrine. Yohimbine behaved as a competitive antagonist of noradrenaline at both low and high concentrations whilst at low concentrations it was non-competitive against phenylephrine. These results suggest a predominance of alpha-1-adrenoceptors in the vas deferens located postjunctionally with a small population of alpha-2-subtype adrenoceptors, whilst the anococcygeus muscle seems to contain relatively more alpha 2-adrenoceptors postjunctionally than the vas deferens.

摘要

用去甲肾上腺素(α-1、α-2激动剂)、去氧肾上腺素(α-1激动剂)、哌唑嗪(α-1拮抗剂)和育亨宾(α-2拮抗剂)对大鼠输精管的α-肾上腺素能受体亚型进行了表征,并与在大鼠肛门尾骨肌中获得的结果进行了比较。在输精管中,哌唑嗪和酚妥拉明都是去甲肾上腺素和去氧肾上腺素的竞争性拮抗剂,而育亨宾无论其浓度如何都是非竞争性拮抗剂。另一方面,在肛门尾骨肌中,低浓度时,哌唑嗪对去甲肾上腺素是非竞争性的,而对去氧肾上腺素是竞争性的。育亨宾在低浓度和高浓度时都是去甲肾上腺素的竞争性拮抗剂,而在低浓度时对去氧肾上腺素是非竞争性的。这些结果表明输精管中α-1肾上腺素能受体占主导地位,位于节后,有少量α-2亚型肾上腺素能受体,而肛门尾骨肌节后似乎比输精管含有相对更多的α-2肾上腺素能受体。

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