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P物质和神经激肽作为人离体膀胱的刺激物。

Substance P and neurokinins as stimulants of the human isolated urinary bladder.

作者信息

Dion S, Corcos J, Carmel M, Drapeau G, Regoli D

机构信息

Department of Pharmacology, Medical School, University of Sherbrooke, Canada.

出版信息

Neuropeptides. 1988 Feb-Mar;11(2):83-7. doi: 10.1016/0143-4179(88)90015-7.

Abstract

Neurokinins are active stimulants of the human isolated urinary bladder. In a preliminary study, performed on bladders taken from four donors, we attempted the characterization of neurokinin receptors. It was shown that neurokinin A is more active than neurokinin B and substance P. Neurokinin receptors selective agonists were also tested and it was found that the most active compound was the NK-A selective agonist, [Nle10]NKA 4-10: A substance P antagonist was able to reduce the effect of neurokinin A but its affinity was rather low. This suggests that the receptor mediating the contraction of the human urinary bladder to neurokinins is of the NK-A (NK2) type. The action of neurokinins on the human urinary bladder appears to be a direct one and mediated by specific receptors different from those of other agents. On the contrary, kinins were found to be active through a new mechanism which was not influenced by either anti-B1 or anti-B2 receptor antagonists.

摘要

神经激肽是人类离体膀胱的活性刺激物。在一项对取自四名供体的膀胱进行的初步研究中,我们尝试对神经激肽受体进行表征。结果表明,神经激肽A比神经激肽B和P物质更具活性。还测试了神经激肽受体选择性激动剂,发现最具活性的化合物是NK-A选择性激动剂[Nle10]NKA 4-10:一种P物质拮抗剂能够降低神经激肽A的作用,但其亲和力相当低。这表明介导人类膀胱对神经激肽收缩反应的受体是NK-A(NK2)型。神经激肽对人类膀胱的作用似乎是直接的,并且由不同于其他介质的特异性受体介导。相反,发现激肽通过一种新机制发挥作用,该机制不受抗B1或抗B2受体拮抗剂的影响。

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