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人血单核细胞中周围型苯二氮䓬受体的特性研究

Characterization of peripheral benzodiazepine receptors in human blood mononuclear cells.

作者信息

Ferrarese C, Appollonio I, Frigo M, Perego M, Pierpaoli C, Trabucchi M, Frattola L

机构信息

Neurological Clinic, University of Milan, Italy.

出版信息

Neuropharmacology. 1990 Apr;29(4):375-8. doi: 10.1016/0028-3908(90)90097-b.

Abstract

In the present study, peripheral-type benzodiazepine receptors in human circulating mononuclear cells were characterized, using [3H]PK 11195 as specific ligand. The specific binding was saturable, with a Bmax of 14 pmol/mg protein and a Kd of 7 nM. The pharmacological characterization, using different displacing drugs, indicated a mitochondrial type of peripheral benzodiazepine receptor since it was not coupled to the GABA receptor and was displaced by protoporphyrin IX. These data indicate that human circulating mononuclear cells possess benzodiazepine recognition sites, similar to non-neuronal receptors. The role of these receptors and possible modifications in different diseases need to be investigated.

摘要

在本研究中,使用[3H]PK 11195作为特异性配体对人循环单核细胞中的外周型苯二氮䓬受体进行了表征。特异性结合是可饱和的,Bmax为14 pmol/mg蛋白质,Kd为7 nM。使用不同的置换药物进行的药理学表征表明,外周苯二氮䓬受体属于线粒体类型,因为它不与GABA受体偶联,且被原卟啉IX置换。这些数据表明,人循环单核细胞具有与非神经元受体相似的苯二氮䓬识别位点。这些受体的作用以及在不同疾病中可能的变化有待研究。

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