PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS IN HUMAN CEREBRAL-CORTEX, KIDNEY, AND COLON

The specific binding of [H-3]PK 11195 and [H-3]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 [H-3]PK 11195 (0.05-10 nM, final concentration) bound with high affinity (K(D) 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 [H-3]Ro 5-4864 (1.25-40 mM, 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 [H-3]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.