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离体人网膜动脉和静脉中节后α-肾上腺素能受体的药理学特性

Pharmacological characterization of postjunctional alpha-adrenoceptors in isolated human omental arteries and veins.

作者信息

Steen S, Skärby T V, Norgren L, Andersson K E

出版信息

Acta Physiol Scand. 1984 Jan;120(1):109-16. doi: 10.1111/j.1748-1716.1984.tb07379.x.

Abstract

The alpha-adrenoceptors in human omental arteries and veins were characterized and compared. In the arteries both prazosin (pA2 9.48) and rauwolscine (pA2 7.19) displaced the noradrenaline (NA) concentration-response (cr) curve towards higher concentrations without reduction of maximum. Neither clonidine, nor oxymetazoline had any consistent contractile effects. Phenylephrine had a lower potency than NA, but a similar intrinsic activity. In the veins, both prazosin (pA2 9.72) and rauwolscine (pA2 8.11) displaced the NA cr-curve towards higher concentrations, but also significantly depressed maximum. Clonidine and oxymetazoline contracted veins from 3 out of 7 and 4 out of 6 patients, respectively. Their pD2-values were similar to that of NA, but their intrinsic activities were significantly lower. NA was more potent than phenylephrine in these vessels, and there was no significant difference in intrinsic activity. The results suggest that in human omental arteries, the postjunctional alpha-adrenoceptors are mainly of the alpha 1-type, even if a small population of alpha 2-adrenoceptors cannot be excluded. In omental veins, there seems to be a functionally important population of postjunctional alpha 2-adrenoceptors occurring together with a population of alpha 1-adrenoceptors.

摘要

对人网膜动脉和静脉中的α-肾上腺素能受体进行了特性鉴定和比较。在动脉中,哌唑嗪(pA2 9.48)和萝芙辛(pA2 7.19)均使去甲肾上腺素(NA)浓度-反应(cr)曲线向高浓度方向移动,且最大反应未降低。可乐定和羟甲唑啉均无一致的收缩作用。去氧肾上腺素的效能低于NA,但内在活性相似。在静脉中,哌唑嗪(pA2 9.72)和萝芙辛(pA2 8.11)均使NA cr曲线向高浓度方向移动,但也显著降低了最大反应。可乐定和羟甲唑啉分别使7例患者中的3例和6例患者中的4例的静脉收缩。它们的pD2值与NA相似,但其内在活性显著较低。在这些血管中,NA比去氧肾上腺素更有效,且内在活性无显著差异。结果表明,在人网膜动脉中,即使不能排除少量α2-肾上腺素能受体,节后α-肾上腺素能受体主要为α1型。在网膜静脉中,似乎存在功能上重要的节后α2-肾上腺素能受体群体,与α1-肾上腺素能受体群体共同存在。

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