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配体与阿片受体结合的分子机制:乙醇的选择性抑制作用?

Molecular mechanisms of ligand binding to opioid receptors: selective inhibition by ethanol?

作者信息

Rapaka R S, Bhargava H N, Renugopalakrishnan V, Collins B J

机构信息

Division of Preclinical Research, National Institute on Drug Abuse, Rockville, MD 20857.

出版信息

NIDA Res Monogr. 1986;75:355-8.

PMID:2828985
Abstract

Effects of varying concentrations of ethanol on the conformations of DAGO, a mu-specific opioid ligand were monitored by FT-IR spectroscopy. The binding of 3H-labeled DAGO (mu-agonist) and DSLET (delta-agonist) to opioid receptors in the presence of varying concentrations of alcohol was also determined. The results indicate that the conformational features of the ligands are altered and conformational factors may play a role in ligand-receptor interaction.

摘要

通过傅里叶变换红外光谱监测不同浓度乙醇对μ特异性阿片样物质配体DAGO构象的影响。还测定了在不同浓度酒精存在下,3H标记的DAGO(μ激动剂)和DSLET(δ激动剂)与阿片受体的结合情况。结果表明,配体的构象特征发生了改变,构象因素可能在配体-受体相互作用中发挥作用。

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