Awad M, Gavish M
Rappaport Family Institute for Research in the Medical Sciences, Bruce Rappaport Faculty of Medicine, Technion-Israel Institute of Technology, Haifa.
Life Sci. 1991;49(16):1155-61. doi: 10.1016/0024-3205(91)90562-p.
The specific binding of [3H]PK 11195 and [3H]Ro 5-4864 to human cerebral cortex, kidney, and colon membranes was studied in order to determine whether peripheral type benzodiazepine receptors (PBR) characteristics located in human tissues are similar to those located in calf or rat tissues. While [3H]PK 11195 (0.05-10 nM, final concentration) bound with high affinity (KD about 2 nM) to human cerebral cortex, kidney, and colon membranes, yielding maximal numbers of binding sites of 255 +/- 23, 1908 +/- 28, and 1633 +/- 98 fmol/mg protein, respectively, the specific binding of [3H]Ro 5-4864 (1.25-40 nM, final concentration), was barely detectable (nonspecific binding about 90% of the total binding). Furthermore, unlabeled PK 11195 was two orders of magnitude more potent than unlabeled Ro 5-4864 in displacing [3H]PK 11195 specific binding from human cerebral cortex and kidney membranes. These results indicate that PBR binding characteristics located in human tissues are similar (but not identical) to those located in calf tissues, but not to those located in rat tissues.
为了确定人体组织中的外周型苯二氮䓬受体（PBR）特性是否与小牛或大鼠组织中的相似，研究了[3H]PK 11195和[3H]Ro 5-4864与人脑皮质、肾脏和结肠膜的特异性结合。虽然[3H]PK 11195（终浓度0.05 - 10 nM）与人脑皮质、肾脏和结肠膜具有高亲和力结合（KD约为2 nM），分别产生最大结合位点数为255±23、1908±28和1633±98 fmol/mg蛋白质，但[3H]Ro 5-4864（终浓度1.25 - 40 nM）的特异性结合几乎检测不到（非特异性结合约占总结合的90%）。此外，在从小脑皮质和肾脏膜上取代[3H]PK 11195特异性结合方面，未标记的PK 11195比未标记的Ro 5-4864强两个数量级。这些结果表明，人体组织中的PBR结合特性与小牛组织中的相似（但不完全相同），但与大鼠组织中的不同。
