卟啉是线粒体（外周型）苯二氮䓬受体的内源性配体。
Porphyrins are endogenous ligands for the mitochondrial (peripheral-type) benzodiazepine receptor.
作者信息
Verma A, Nye J S, Snyder S H
出版信息
Proc Natl Acad Sci U S A. 1987 Apr;84(8):2256-60. doi: 10.1073/pnas.84.8.2256.
Abstract
"Peripheral-type" benzodiazepine receptors are localized to the outer mitochondrial membrane. We have identified potent competitive inhibitors of these receptors and purified them from human blood and from several rat organs. TLC analysis of the purified inhibitor from erythrocytes displays a single peak of inhibitory activity with an absorbance spectrum identical to hemin. All of the inhibitory activity in extracts of several tissues can be accounted for by their porphyrin and metalloporphyrin content. Pure hemin and protoporphyrin IX competitively inhibit mitochondrial benzodiazepine binding with Ki values of 41 and 15 nM, respectively, and are less active by a factor of 1000 at central-type benzodiazepine receptors. Thus, porphyrins appear to be endogenous ligands for mitochondrial benzodiazepine receptors.
摘要
“外周型”苯二氮䓬受体定位于线粒体外膜。我们已鉴定出这些受体的强效竞争性抑制剂，并从人血和几种大鼠器官中纯化出了它们。对红细胞中纯化的抑制剂进行薄层层析分析，显示出单一的抑制活性峰，其吸收光谱与血红素相同。几个组织提取物中的所有抑制活性都可由其卟啉和金属卟啉含量来解释。纯血红素和原卟啉IX分别以41和15 nM的Ki值竞争性抑制线粒体苯二氮䓬结合，在中枢型苯二氮䓬受体上的活性则低1000倍。因此，卟啉似乎是线粒体苯二氮䓬受体的内源性配体。
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