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多种阿片受体:酒精选择性抑制与δ受体的结合。

Multiple opiate receptors: alcohol selectively inhibits binding to delta receptors.

作者信息

Hiller J M, Angel L M, Simon E J

出版信息

Science. 1981 Oct 23;214(4519):468-9. doi: 10.1126/science.6270788.

Abstract

The addition of ethanol or other aliphatic alcohols to rat brain membranes strongly inhibits binding of enkephalins at concentrations at which little inhibition of opiate alkaloids is seen. Inhibition is reversible, and potency increases with chain length of the alcohol. The results suggest that delta receptors are considerably more sensitive to alcohols than mu receptors. This is the first demonstration of selective inhibition of one of the postulated classes of opiate receptors by a reagent that is not a ligand for the receptor.

摘要

向大鼠脑膜中添加乙醇或其他脂肪醇,在对阿片生物碱几乎没有抑制作用的浓度下,能强烈抑制脑啡肽的结合。抑制作用是可逆的,且效力随醇链长度增加而增强。结果表明,δ受体对醇的敏感性远高于μ受体。这是首次证明一种并非受体配体的试剂对假定的阿片受体类别之一具有选择性抑制作用。

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