血管活性肽及其受体。

Blood vessels Pub Date : 1990-01-01 DOI:10.1159/000158804
D Regoli, S Dion, N E Rhaleb, G Drapeau, P D'Orléans-Juste
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引用次数: 22

摘要

多肽作为血管收缩剂(如血管紧张素、血管加压素)或血管舒张剂(血管收缩素、神经收缩素),通过直接激活血管平滑肌中的特定受体或间接通过释放其他内源性血管张力抑制剂。本研究分析了激肽和神经激肽及其多种受体,以评估多肽对血管舒张的可能贡献。利用新的选择性激动剂和拮抗剂,已经对激肽受体B1和B2进行了表征。B1和B2受体存在于犬和兔多种离体血管的内皮(B2)和平滑肌(B2, B1)中,在那里它们具有刺激和抑制作用。血管舒张剂抑制机制依赖于内皮松弛因子和/或前列腺素从内皮或平滑肌的释放,特别是在狗肾血管中,B1和B2受体似乎都参与引起血管舒张。B2受体也被证明通过直接作用于感觉纤维或心外膜反射区来激活心血管反射。三种类型的神经激肽受体,即NK-1, NK-2和NK-3,已经通过使用天然存在的肽和一些类似物作为单一受体类型的选择性激动剂被鉴定出来。NK-1受体(对P物质特别敏感)已被证明存在于内皮中,它们促进内皮松弛因子的释放,而NK-2受体(对神经激肽A敏感)存在于兔的肺动脉中,并直接作用于平滑肌收缩。(摘要删节250字)
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Vasoactive peptides and their receptors.

Peptides act as vasoconstrictors (for instance angiotensins, vasopressin) or vasodilators (the kinins, the neurokinins), both through direct activation of specific receptors in the vascular smooth muscles or indirectly through the release of other endogenous inhibitors of the vascular tone. Kinins and neurokinins as well as their multiple receptors have been analyzed in the present study to assess the possible contributions of peptides to vasodilatation. Kinin receptors, B1 and B2, have been characterized, using new selective agonists and antagonists. B1 and B2 receptors appear to present in endothelium (B2) and in smooth muscles (B2, B1) of a variety of isolated vessels of the dog and the rabbit, where they subserve both stimulatory and inhibitory effects. Vasodilator inhibitory mechanisms depend on the release of the endothelium-relaxing factor and/or of prostanoids from the endothelium or the smooth muscles, especially in the dog renal vessels, where both B1 and B2 receptors appear to be involved in causing vasodilatation. B2 receptors have also been shown to activate cardiovascular reflexes through a direct action on sensory fibers or on reflexogenic areas of the epicardium. Three types of receptors for neurokinins, namely NK-1, NK-2 and NK-3, have been identified by the use of naturally occurring peptides and of some analogues that act as selective agonists of a single receptor type. NK-1 receptors (particularly sensitive to substance P) have been shown to be present in endothelia where they promote the release of the endothelium relaxing factor, while NK-2 receptors (sensitive to neurokinin A) are found in the pulmonary artery of the rabbit and act directly to contract the smooth muscle.(ABSTRACT TRUNCATED AT 250 WORDS)

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