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新型非肽类NK1受体拮抗剂CP-96,345对豚鼠气道神经源性血浆渗出的抑制作用

Inhibition of neurogenic plasma exudation in guinea-pig airways by CP-96,345, a new non-peptide NK1 receptor antagonist.

作者信息

Lei Y H, Barnes P J, Rogers D F

机构信息

Department of Thoracic Medicine, National Heart & Lung Institute, London.

出版信息

Br J Pharmacol. 1992 Feb;105(2):261-2. doi: 10.1111/j.1476-5381.1992.tb14243.x.

DOI:10.1111/j.1476-5381.1992.tb14243.x
PMID:1373095
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1908658/
Abstract

A new non-peptide tachykinin antagonist, CP-96,345, inhibited airway plasma exudation induced in guinea-pigs by i.v. substance P in a dose-dependent manner with dose-ratios in the main bronchi of 5 at 1 nmol kg-1 and 19 at 100 nmol kg-1. At 100 nmol kg-1, CP-96,345 completely inhibited plasma exudation induced by either electrical stimulation of the cervical vagus nerves or i.v. capsaicin, indicating inhibition of the effects of endogenous tachykinins, but did not inhibit the bronchoconstrictor response to neurokinin A, suggesting selectivity for NK1 receptors. CP-96,345 may be useful in examining the role of endogenous tachykinins in vivo.

摘要

一种新的非肽类速激肽拮抗剂CP - 96,345，能剂量依赖性地抑制静脉注射P物质诱导的豚鼠气道血浆渗出，在主支气管中，1 nmol kg-1时的剂量比为5，100 nmol kg-1时为19。在100 nmol kg-1时，CP - 96,345完全抑制了由颈迷走神经电刺激或静脉注射辣椒素诱导的血浆渗出，表明其抑制了内源性速激肽的作用，但不抑制对神经激肽A的支气管收缩反应，提示其对NK1受体具有选择性。CP - 96,345可能有助于研究内源性速激肽在体内的作用。