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苯并吗啡烷选择性(κ)位点的个体发生:计算机化分析

Ontogeny of benzomorphan-selective (kappa) sites: a computerized analysis.

作者信息

Spain J W, Bennett D B, Roth B L, Coscia C J

出版信息

Life Sci. 1983;33 Suppl 1:235-8. doi: 10.1016/0024-3205(83)90486-1.

Abstract

In an investigation of the postnatal development of kappa opiate receptors, the affinity and capacity of 0.5 nM [3H]-ethylketocyclazocine (EKC) binding in crude rat brain homogenates was measured by displacement with unlabeled EKC, morphine, or D-ala2-D-leu5-enkephalin (DADL). Displacement curves were analyzed using a weighted, non-linear regression, curve fitting computer program. At all stages of development, [3H]-EKC binding fit a two site model significantly better than a one site model. Affinities of EKC, morphine, or DADL for the high affinity [3H]-EKC binding site did not change during the postnatal period. The density of the high affinity [3H]-EKC binding site increased linearly with age, whereas the levels of the low affinity site rose more rapidly during the second week.

摘要

在一项关于κ阿片受体产后发育的研究中,通过用未标记的EKC、吗啡或D-ala2-D-leu5-脑啡肽(DADL)进行置换,测量了粗制大鼠脑匀浆中0.5 nM [3H]-乙基酮环唑辛(EKC)结合的亲和力和容量。使用加权非线性回归曲线拟合计算机程序分析置换曲线。在发育的所有阶段,[3H]-EKC结合符合双位点模型,明显优于一位点模型。EKC、吗啡或DADL对高亲和力[3H]-EKC结合位点的亲和力在产后期间没有变化。高亲和力[3H]-EKC结合位点的密度随年龄呈线性增加,而低亲和力位点的水平在第二周上升得更快。

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