兔小脑μ阿片受体的表征与分布

Characterization and distribution of mu opioid receptors in rabbit cerebellum.

作者信息

Lu Y F, Li G F, Chi Z Q

机构信息

Shanghai Joint Laboratory of Life Sciences, Chinese Academy of Sciences.

出版信息

Zhongguo Yao Li Xue Bao. 1993 Nov;14(6):489-91.

PMID:8010044

Abstract

The binding characteristics and distributions of [3H]ohmefentanyl ([3H]OMF), [3H]etorphine, [3H] N-methyl-N-[7-(I-pyrrolidinyl)-1-oxaspiro(4,5)dec-7-yl] benzeneacetamide [3H]U-69593), and [3H] (D-penicillamine2, D-penicillamine5) enkephalin ([3H]DPDPE) in rabbit cerebellum were studied. In saturation experiment, [3H]OMF bound to a single population of sites with Kd = 2.2 +/- 1.3 nmol.L-1 and Bmax = 69 +/- 13 fmol/mg protein. The results of [3H]etorphine (Kd = 1.0 +/- 0.4 nmol.L-1 and Bmax = 16 +/- 6 fmol/mg protein) were similar to those of [3H]OMF. There were no specific bindings of [3H]U-69593 and [3H]DPDPE in rabbit cerebellar membranes. In autoradiographic study, the gray scales of specific binding for [3H]OMF, [3H]etorphine, [3H]U-69593, and [3H]DPDPE were 20.2 +/- 4.6, 8.5 +/- 2.7, 2.0 +/- 0.7, and 3.2 +/- 4.3, respectively. The gray matter of rabbit cerebellum was intensely labeled by [3H]OMF and [3H]etorphine, but not by [3H]U-69593 or [3H]DPDPE. These results suggested that the rabbit cerebellum contained mu opioid receptors.

摘要

研究了[3H]奥米芬太尼（[3H]OMF）、[3H]埃托啡、[3H]N-甲基-N-[7-(1-吡咯烷基)-1-氧杂螺(4,5)癸-7-基]苯乙酰胺（[3H]U-69593）和3H脑啡肽（[3H]DPDPE）在兔小脑内的结合特性及分布情况。在饱和实验中，[3H]OMF与单一类位点结合，解离常数（Kd）为2.2±1.3 nmol·L-1，最大结合容量（Bmax）为69±13 fmol/mg蛋白。[3H]埃托啡（Kd = 1.0±0.4 nmol·L-1，Bmax = 16±6 fmol/mg蛋白）的结果与[3H]OMF相似。[3H]U-69593和[3H]DPDPE在兔小脑膜中无特异性结合。在放射自显影研究中，[3H]OMF、[3H]埃托啡、[3H]U-69593和[3H]DPDPE特异性结合的灰度值分别为20.2±4.6、8.5±2.7、2.0±0.7和3.2±4.3。兔小脑灰质被[3H]OMF和[3H]埃托啡强烈标记，但未被[3H]U-69593或[3H]DPDPE标记。这些结果表明兔小脑含有μ阿片受体。