Peripheral-Type Benzodiazepine/Diazepam Binding Inhibitor Receptor: Biological Role in Steroidogenic Cell Function*
Abstract
BENZODIAZEPINES, a class of drugs that includes compounds such as diazepam (Valium), are frequently prescribed because of their anxiolytic, anticonvulsant, musclerelaxant, and hypnotic properties. It has been shown that the pharmacological effects of benzodiazepines are mediated via a specific receptor complex located in the central nervous system (CNS); benzodiazepines bind to a domain that allosterically regulates chloride channel gating by γ-aminobutyric acid (GABA), on GABAA receptors (1–3). In 1977, while searching for specific benzodiazepine receptors, Braestrup and Squires (4) observed the presence of high density radiolabeled diazepam binding sites in the kidney. Since then, numerous papers have reported that this class of benzodiazepine binding sites is present apparently in all tissues examined including the CNS (Section III). Because of their abundance in peripheral tissues and in order to distinguish them from the GABAA or central benzodiazepine receptors, this class of benzodiazepine binding sites was named “peripheral-type benzodiazepine-type benzodiazepine binding sites.” Moreover, in the last 5 yr several studies reported physiological roles for these binding sites and they were then termed “peripheraltype benzodiazepine receptors” (PBRs) (5–8). However, there are a number of names that have been assigned to this receptor:
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Substantial data indicate that the action of StAR also requires the translocator protein, TSPO, on the OMM.
“Substantial data indicate that the action of StAR also requires the translocator protein, TSPO (also known as the peripheral benzodiazepine receptor) on the OMM (83-85).”
From The Molecular Biology, Biochemistry, and Physiology of Human Steroidogenesis and Its Disorders (2011) · cites this paper as [83]
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- Authors
- PAPADOPOULOS, V.
- Affiliations
- Georgetown University Medical Center (US)
- Corresponding author
- PAPADOPOULOS, VASSILIOS
- Venue
- Endocrine Reviews
- Publisher
- The Endocrine Society
- Published
- 1993-04
- Volume
- 14
- Issue
- 2
- Pages
- 222-240
- ISSN
- 0163-769X (ISSN-L)
- 1945-7189
- OpenAlex
- W1979263239
- Cited by
- 417
- References
- 0
- Citations by year
- 2025: 2 · 2024: 2 · 2023: 2 · 2022: 4 · 2021: 2 · 2019: 3 · 2018: 4 · 2017: 4 · 2016: 6 · 2015: 6 · 2014: 7 · 2013: 4 · 2012: 16
- FWCI
- 8.30
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrine Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (1r55dk043358-01a1)
- National Institute of Diabetes and Digestive and Kidney Diseases (DK43358)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- translocator protein (TSPO), steroidogenesis, steroidogenic cells, GABAA receptor, receptor nomenclature, steroidogenic enzyme regulation
- MeSH terms
- Amino Acid Sequence, Animals, Carrier Proteins, Cell Division, Gene Expression Regulation, Humans, Ligands, Molecular Sequence Data, Porphyrins, Receptors, GABA-A, Steroids, Sequence Homology, Amino Acid, Diazepam Binding Inhibitor
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