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[3H]TCP:一种对大鼠脑内苯环己哌啶受体具有高亲和力的新工具。

[3H]TCP: a new tool with high affinity for the PCP receptor in rat brain.

作者信息

Vignon J, Chicheportiche R, Chicheportiche M, Kamenka J M, Geneste P, Lazdunski M

出版信息

Brain Res. 1983 Nov 28;280(1):194-7. doi: 10.1016/0006-8993(83)91193-9.

Abstract

PCP binding sites have previously been demonstrated in the central nervous system with [3H]PCP. We now describe the binding properties to rat brain membranes of [3H]TCP, a PCP derivative. It is very advantageous to use [3H]TCP instead of [3H]PCP for the 3 following reasons: (i) it has a better affinity (Kd = 7.4 nM) for PCP binding sites than PCP itself; (ii) it dissociates slowly from its binding sites (t 1/2 = 20 min); (iii) the non-specific binding component obtained with [3H]TCP is much lower than that found with [3H]PCP.

摘要

以前曾用[3H]苯环己哌啶在中枢神经系统中证实了苯环己哌啶结合位点。我们现在描述了一种苯环己哌啶衍生物[3H]三甲氧苯乙哌啶与大鼠脑膜的结合特性。使用[3H]三甲氧苯乙哌啶而非[3H]苯环己哌啶有以下三个非常有利的原因:(i) 它对苯环己哌啶结合位点的亲和力(Kd = 7.4 nM)比苯环己哌啶本身更好;(ii) 它从结合位点解离缓慢(半衰期 = 20分钟);(iii) 用[3H]三甲氧苯乙哌啶获得的非特异性结合成分比用[3H]苯环己哌啶发现的要低得多。

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