Characterization of peripheral benzodiazepine receptors in rat prostatic adenocarcinoma

Using PK 11195, a high affinity ligand for peripheral benzodiazepine receptors (PBZr), binding sites in isolated mitochondrial (m-fraction) and microsomal fractions (p-fraction) from R-3327 Dunning AT-1 tumors, ventral and dorsolateral prostate were studied. Binding of PK 11195 in both m- and p-fractions from AT-1 tumors, but only in m-fraction from ventral and dorsolateral prostate, was specific, saturable, and of high affinity. The PBZr density in m-fraction from AT-1 tumors was 6-fold and 20-fold higher than that in ventral and dorsolateral prostate, respectively. The receptor density in p-fraction from AT-1 tumors was approximately 25% of that found in the m-fraction. Clear differences were observed in the competition by both diazepam and flunitrazepam for binding sites in m- and p-fractions from tumors. These data indicate that the receptors were not only localized to the mitochondria, but were also present in considerable amounts in the microsomal fractions. The unusually high amounts of receptors in the fast growing anaplastic prostatic tumor suggest their involvement in the regulation of cell proliferation and possibly in tumorigenesis. © 1994 Wiley-Liss, Inc.