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外周型苯二氮受体位于线粒体膜上 ,参与构成线粒体膜透性转变孔 ,调节线粒体跨膜电位和电子传递链呼吸功能。地西泮通过与外周型苯二氮受体结合 ,调节线粒体膜透性转变孔不同水平的开放 ,从而 ,调控线粒体膜内外细胞信号传导和类固醇的转运 ,表现出抗焦虑、抗癫痫、抗炎、抑制肿瘤以及浓度依赖的细胞毒性等效应。本文综述了外周型苯二氮受体的分子结构和生理功能及其介导的地西泮药理毒理作用研究进展。
Peripheral benzodiazepine receptors are located on the mitochondrial membrane and are involved in the formation of mitochondrial membrane permeability transitional pores that regulate the mitochondrial transmembrane potential and the respiratory function of the electron transport chain. Diazepam modulates the openness of mitochondrial membrane permeability transitional pores by binding to peripheral benzodiazepine receptors and thereby modulates mitochondrial intracellular and extracellular signal transduction and steroid transport, exhibiting anxiolytic, antiepileptic, and anti-epileptic effects Inflammation, tumor suppression and concentration-dependent cytotoxic effects. This review summarizes the molecular structure and physiological functions of peripheral benzodiazepine receptors and the progress in their pharmacological and toxicological effects mediated by diazepam.