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Autoradiographic localisation of benzodiazepine receptors in the brains of humans and animals

Abstract

THE benzodiazepine (BZ) drugs are used as anxiolytics, hypnotics, anticonvulsants and muscle relaxants. They are the most widely prescribed of all psychotropic drugs and seem to exert their action by binding to a specific receptor site on brain membranes1–2. This receptor appears to interact with neurotransmission mediated by γ-aminobutyric acid (GABA)3–8. Biochemical studies of BZ receptor distributions in brain reveal large regional variations9,10. An increase in resolution of localisation of BZ receptors would provide greater insight into mechanisms of actions of BZs. In this study, we report for the first time the light microscopic autoradiographic localisation of BZ receptors in mammalian central nervous system (CNS) and, to our knowledge, the first receptor autoradiography in human brain tissue. We observed striking variations in receptor densities in different areas which, in some cases, were species dependent.

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YOUNG, W., KUHAR, M. Autoradiographic localisation of benzodiazepine receptors in the brains of humans and animals. Nature 280, 393–395 (1979). https://doi.org/10.1038/280393a0

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