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阿片类药物对大鼠肾脏中³H-EKC结合的置换作用:与利尿活性的相关性

Displacement of 3H-EKC binding by opioids in rat kidney: a correlate to diuretic activity.

作者信息

Slizgi G R, Ludens J H

出版信息

Life Sci. 1985 Jun 10;36(23):2189-93. doi: 10.1016/0024-3205(85)90328-5.

DOI:10.1016/0024-3205(85)90328-5
PMID:2860552
Abstract

Multiple opioid binding sites have been documented in brain tissue. In this study we report on the presence of binding sites for the opioid ethylketocyclazocine (EKC) in a membrane fraction of rat kidney. Binding appeared to be selective in that opioids varied markedly in their capacities to displace 3H-EKC. Correlating with the capacity of an opioid to displace 3H-EKC was the ability to produce diuresis. Although our studies cannot assign a particular physiological or pharmacological role for the renal EKC binding sites, binding studies of this nature may, nonetheless, be a means by which diuretic activity of opioids can be predicted.

摘要

在脑组织中已证实存在多个阿片样物质结合位点。在本研究中,我们报告了在大鼠肾脏膜组分中存在阿片样物质乙基酮环唑辛(EKC)的结合位点。结合似乎具有选择性,因为不同阿片样物质置换³H-EKC的能力差异显著。阿片样物质置换³H-EKC的能力与其产生利尿作用的能力相关。虽然我们的研究无法确定肾脏EKC结合位点的特定生理或药理作用,但这种性质的结合研究可能是预测阿片样物质利尿活性的一种手段。

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引用本文的文献

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Influence of asimadoline, a new kappa-opioid receptor agonist, on tubular water absorption and vasopressin secretion in man.
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