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亮氨酸脑啡肽非竞争性抑制[3H]纳洛酮与阿片μ-识别位点的结合:体外δ----μ结合位点相互作用的证据。

Leucine enkephalin noncompetitively inhibits the binding of [3H]naloxone to the opiate mu-recognition site: evidence for delta----mu binding site interactions in vitro.

作者信息

Rothman R B, Danks J A, Jacobson A E, Burke T R, Rice K C

出版信息

Neuropeptides. 1985 Jul;6(4):351-63. doi: 10.1016/0143-4179(85)90008-3.

Abstract

Using quantitative methods, this study examined the hypothesis that delta-ligands are noncompetitive inhibitors at a population of mu-binding sites. Evidence is presented that with the defined set of in vitro assay conditions utilized, [3H]naloxone labels two binding sites: the mu binding site and a second site tentatively identified as a kappa binding site, and that leucine enkephalin is a noncompetitive inhibitor at the mu recognition site.

摘要

本研究采用定量方法检验了δ-配体在一群μ-结合位点上为非竞争性抑制剂的假说。结果表明,在所使用的特定体外试验条件下,[3H]纳洛酮标记了两个结合位点:μ-结合位点和另一个暂定为κ-结合位点的位点,并且亮氨酸脑啡肽在μ-识别位点上为非竞争性抑制剂。

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