神经激肽对兔主动脉的内皮依赖性舒张作用由NK1受体介导。

Endothelium-dependent relaxant effect of neurokinins on rabbit aorta is mediated by the NK1 receptor.

作者信息

Rubino A, Thomann H, Henlin J M, Schilling W, Criscione L

机构信息

Cardiovascular Research Department, Ciba-Geigy Ltd., Basle, Switzerland.

出版信息

Eur J Pharmacol. 1992 Mar 3;212(2-3):237-40. doi: 10.1016/0014-2999(92)90335-2.

DOI:10.1016/0014-2999(92)90335-2

PMID:1318213

Abstract

Several neurokinins, namely substance P, neurokinin A, neurokinin B, [beta-Ala8]neurokinin A-(4-10) and senktide, were tested on noradrenaline-precontracted rabbit aortic rings to characterize the receptor mediating their endothelium-dependent relaxant effect in this preparation. CP-96,345, the new nonpeptide antagonist selective for the NK1 receptor, was also studied. Substance P, neurokinin A and neurokinin B, in that order of potency, were effective in relaxing precontracted rings, indicating the involvement of the NK1 receptor; [beta-Ala8]neurokinin A-(4-10) and senktide, which are selective agonists for NK2 and NK3 receptors, respectively, had no significant relaxant effect. The relaxant effects of substance P, neurokinin A and neurokinin B were competitively antagonized by nanomolar concentrations of CP-96,345. These findings support the view that the NK1 receptor mediates the endothelium-dependent relaxant effect of the neurokinins in rabbit aorta.

摘要

在去甲肾上腺素预收缩的兔主动脉环上测试了几种神经激肽，即P物质、神经激肽A、神经激肽B、[β-丙氨酸8]神经激肽A-(4-10)和senktide，以表征介导它们在此制剂中内皮依赖性舒张作用的受体。还研究了对NK1受体具有选择性的新型非肽拮抗剂CP-96,345。P物质、神经激肽A和神经激肽B按效力顺序有效地舒张了预收缩的血管环，表明NK1受体参与其中；[β-丙氨酸8]神经激肽A-(4-10)和senktide分别是NK2和NK3受体的选择性激动剂，没有明显的舒张作用。P物质、神经激肽A和神经激肽B的舒张作用被纳摩尔浓度的CP-96,345竞争性拮抗。这些发现支持NK1受体介导神经激肽在兔主动脉中内皮依赖性舒张作用的观点。