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离子条件在体外对3H-DADL与I型和II型阿片δ受体的结合有不同影响。

Ionic conditions differentially affect 3H-DADL binding to type-I and type-II opiate delta receptors in vitro.

作者信息

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

出版信息

Neuropeptides. 1984 May;4(3):261-8. doi: 10.1016/0143-4179(84)90108-2.

Abstract

It is widely accepted that the prototypic delta agonist DADL (D-ala2-D-leu5-enkephalin) labels two binding sites in vitro. Using the site directed, receptor selective alkylating agents, BIT and FIT (Rice et al.. Science 220:314-316, 1983), we recently described (Rothman et al, Neuropeptides, in press) the preparation of membranes possessing only lower affinity 3H-DADL binding sites (FIT-treated membranes, type-I delta sites) as well as membranes greatly enriched with higher affinity binding sites (BIT-treated membranes, type-II delta sites). In this paper we report that ionic conditions differentially affect the binding of 3H-DADL to FIT- and BIT-treated membranes, supporting the notion that 3-H-DADL labels two distinct delta binding sites.

摘要

人们普遍认为,典型的δ激动剂DADL(D-ala2-D-leu5-脑啡肽)在体外标记两个结合位点。利用位点定向、受体选择性烷基化剂BIT和FIT(Rice等人,《科学》220:314 - 316,1983),我们最近描述了(Rothman等人,《神经肽》,即将发表)仅具有较低亲和力3H-DADL结合位点的膜的制备(FIT处理的膜,I型δ位点)以及富含较高亲和力结合位点的膜(BIT处理的膜,II型δ位点)。在本文中,我们报告离子条件对3H-DADL与FIT和BIT处理的膜的结合有不同影响,支持3-H-DADL标记两个不同δ结合位点的观点。

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