PMID: 7542903Jun 1, 1995Paper

Hormonal regulation of peripheral-type benzodiazepine receptors

The Journal of Steroid Biochemistry and Molecular Biology
M Gavish

Abstract

Central benzodiazepine (BZ) receptors are located only in the central nervous system and mediate the clinical effects obtained by various BZs. In addition, there is another receptor that binds BZs with different drug specificities, which is located mainly on the outer mitochondrial membrane of various peripheral tissues. Peripheral BZ receptors (PBR) are composed of three subunits: an isoquinoline binding site, a voltage-dependent anion channel, and an adenine nucleotide carrier, with molecular weights of 18, 32, and 30 kDa, respectively. Complementary DNA of the isoquinoline binding subunit has been cloned in rat, calf, and human. The major role of PBR is in the regulation of steroid biosynthesis. Various PBR ligands stimulate the conversion of cholesterol into pregnenolone and the production of steroid hormones. The naturally occurring diazepam-binding inhibitor stimulates in vivo steroidogenesis via binding to PBR. In the female, PBR density is increased in rat and human ovary proportional with greater cell maturation and differentiation. In the male, testosterone modulates PBR density in the genital tract. These results show the strong relationship between PBR and the endocrine system.

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Citations

Apr 29, 1996·European Journal of Pharmacology·M K YiuM P Ngan
Mar 19, 2002·Biophysical Chemistry·Daniel A García, María A Perillo
Jan 28, 2010·American Journal of Physiology. Endocrinology and Metabolism·Homayoun Sadeghi, Hugh S Taylor
Apr 21, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Anna SantoroRosaria Meli

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