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[3H]-SKF 10047与大鼠脑膜的结合:κ异受体的证据。

[3H]-SKF 10047 binding to rat brain membranes: evidence for kappa isoreceptors.

作者信息

Pilapil C, Wood P L

出版信息

Life Sci. 1983;33 Suppl 1:263-5. doi: 10.1016/0024-3205(83)90493-9.

Abstract

Studies of the binding of [3H]-SKF10047 to rat brain membrane preparations revealed a binding site which possessed high affinity for kappa and agonist/antagonist analgesics. However, this site was distinguished from kappa sites labelled with [3H]-ethylketazocine by its high affinity for Met5-enkephalin Arg6.Phe7 and beta-endorphin as well as its low affinity for dynorphin 1-13. We therefore tentatively suggest that this may represent a possible kappa isoreceptor population.

摘要

对[3H]-SKF10047与大鼠脑膜制剂结合的研究揭示了一个对κ和激动剂/拮抗剂镇痛药具有高亲和力的结合位点。然而,该位点与用[3H]-乙基酮唑辛标记的κ位点不同,它对甲硫氨酸脑啡肽Arg6.Phe7和β-内啡肽具有高亲和力,而对强啡肽1-13具有低亲和力。因此,我们初步认为这可能代表了一种可能的κ异受体群体。

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