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β-内啡肽拮抗剂的阿片受体选择性研究。

Studies on opioid receptor selectivity of beta-endorphin antagonists.

作者信息

Hammonds R G, Li C H

出版信息

Int J Pept Protein Res. 1985 Aug;26(2):118-20. doi: 10.1111/j.1399-3011.1985.tb03188.x.

Abstract

Opioid receptor selectivity of several beta-endorphin (beta-EP) analogs which antagonize beta-EP-induced analgesia has been assessed using partially selective binding assays. Although the apparent affinity dissociation constant of beta-EP in these assays varies from 0.2 to 360 nm, the potency of beta-EP antagonists relative to beta-EP remains largely unchanged. It is unlikely that differences in receptor affinities can account for the antagonist properties of these analogs in vivo.

摘要

使用部分选择性结合试验评估了几种拮抗β-内啡肽(β-EP)诱导镇痛作用的β-内啡肽类似物的阿片受体选择性。尽管在这些试验中β-EP的表观亲和力解离常数在0.2至360 nM之间变化,但β-EP拮抗剂相对于β-EP的效力基本保持不变。受体亲和力的差异不太可能解释这些类似物在体内的拮抗特性。

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