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人离体股静脉和动脉中接头后α-肾上腺素能受体的特性研究

Characterisation of postjunctional alpha-adrenoceptors in isolated human femoral veins and arteries.

作者信息

Glusa E, Markwardt F

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1983 Jun;323(2):101-5. doi: 10.1007/BF00634256.

Abstract

In order to characterise the pharmacological properties of postjunctional alpha-adrenoceptors, both the contractile effects of alpha-adrenoceptor agonists and the blocking potencies of selective alpha-adrenoceptor antagonists were studied in isolated human femoral veins and arteries. The veins were more sensitive to noradrenaline than the arteries. Guanfacine had a higher intrinsic activity in veins than in arteries, whereas the reverse was true for phenylephrine. The antagonists rauwolscine and yohimbine were more potent against noradrenaline in the veins than in arteries, while corynanthine was equally potent in either tissue. They antagonised the noradrenaline response in a competitive manner. Prazosin proved to be the most potent competitive antagonist in arteries, while in veins it exerted weak and non-competitive antagonism. The results suggest that the alpha-adrenoceptor population at the postjunctional site differs between human femoral veins and arteries. The veins seem to contain more alpha 2- than alpha 1-adrenoceptors postjunctionally, whereas in the arteries the alpha 1-subtype prevails. The results indicate the possibility of influencing selectively adrenergic reactions in the capacitance and resistance vessels.

摘要

为了描述接头后α-肾上腺素能受体的药理学特性,在离体人股静脉和动脉中研究了α-肾上腺素能受体激动剂的收缩作用以及选择性α-肾上腺素能拮抗剂的阻断效能。静脉对去甲肾上腺素比动脉更敏感。胍法辛在静脉中的内在活性高于动脉,而苯肾上腺素则相反。拮抗剂萝芙辛和育亨宾对静脉中去甲肾上腺素的作用比对动脉更强,而育亨宾在两种组织中的效能相同。它们以竞争性方式拮抗去甲肾上腺素反应。哌唑嗪被证明是动脉中最有效的竞争性拮抗剂,而在静脉中它表现出微弱的非竞争性拮抗作用。结果表明,人股静脉和动脉接头后部位的α-肾上腺素能受体群体不同。静脉接头后似乎含有更多的α2-而非α1-肾上腺素能受体,而在动脉中α1-亚型占主导。结果表明有可能选择性地影响容量血管和阻力血管中的肾上腺素能反应。

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