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阿片类药物结合位点的浓度和分布的物种差异。

Species differences in the concentrations and distributions of opioid binding sites.

作者信息

Robson L E, Gillan M G, Kosterlitz H W

出版信息

Eur J Pharmacol. 1985 May 28;112(1):65-71. doi: 10.1016/0014-2999(85)90239-0.

Abstract

Binding at the mu, delta- and kappa-types of opioid binding sites was compared in homogenates from the brains of guinea-pig, rabbit, rat and two mouse strains, under conditions of selective labelling. Species differences were shown by two observations. Firstly, analysis of saturation curves in homogenates of brain from which the cerebellum had been removed showed that in guinea-pig brain the opioid binding sites consist of 24% mu-sites, 32% delta-sites and 44% kappa-sites. In contrast, in rabbit brain the corresponding values are 43% mu-sites, 19% delta-sites and 37% kappa-sites and in rat brain, 46% mu-sites, 42% delta-sites and 12% kappa-sites. In the brains of DBA/2 mice the opioid binding sites are comprised of 51% mu-sites, 29% delta-sites and 20% kappa-sites and in C57BL/10 mice, of 44% mu-sites, 35% delta-sites and 21% kappa-sites; these strain differences are due to significant differences in the concentrations of the mu-sites. Secondly, species differences were found when the binding of single concentrations of tritiated ligands (1 X KD value in whole brain) was determined at mu-, delta- and kappa-sites in six brain regions from guinea-pig, rat or rabbit.

摘要

在选择性标记条件下,比较了豚鼠、兔子、大鼠和两种小鼠品系大脑匀浆中μ、δ和κ型阿片样物质结合位点的结合情况。通过两项观察发现了物种差异。首先,对去除小脑的大脑匀浆中的饱和曲线进行分析表明,在豚鼠大脑中,阿片样物质结合位点由24%的μ位点、32%的δ位点和44%的κ位点组成。相比之下,在兔子大脑中,相应的值分别为43%的μ位点、19%的δ位点和37%的κ位点;在大鼠大脑中,为46%的μ位点、42%的δ位点和12%的κ位点。在DBA/2小鼠大脑中,阿片样物质结合位点由51%的μ位点、29%的δ位点和20%的κ位点组成;在C57BL/10小鼠中,为44%的μ位点、35%的δ位点和21%的κ位点;这些品系差异是由于μ位点浓度的显著差异所致。其次,当在豚鼠、大鼠或兔子的六个脑区的μ、δ和κ位点测定单一浓度的氚化配体(全脑1×KD值)的结合情况时,发现了物种差异。

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