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An endogenous protein modulates the affinity of GABA and benzodiazepine receptors in rat brain

Nature volume 275, pages 553–555 (1978)Cite this article

Abstract

BIOCHEMICAL1,2 and neurophysiological3–5 evidence has suggested that benzodiazepines may relieve anxiety facilitating the synaptic action of γ-aminobutyric acid (GABA), an important neurotransmitter in the brain of mammals, including man. As benzodiazepines fail to increase the turnover of GABA stored presynaptically as would be expected if they were to act as indirect GABA agonists, and since it has been difficult to demonstrate a direct agonistic action of the benzodiazepines on GABA postsynaptic receptors5–7 in vitro, the molecular mechanism whereby benzodiazepines facilitate GABAergic transmission is still unknown. Independent investigators8–10 have recently reported the presence of a high affinity, saturable, stereospecific binding site for benzodiazepines in synaptic membrane preparations obtained from brain of different animal species, including man. This high affinity binding is now used to determine the therapeutic potency and to study the mode of action of benzodiazepines in anxiety.

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Authors and Affiliations

  1. Laboratory of Preclinical Pharmacology, National Institute of Mental Health, Saint Elizabeths Hospital, Washington, D.C., 20032

    A. GUIDOTTI, G. TOFFANO & E. COSTA

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  1. A. GUIDOTTI
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  2. G. TOFFANO
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  3. E. COSTA
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GUIDOTTI, A., TOFFANO, G. & COSTA, E. An endogenous protein modulates the affinity of GABA and benzodiazepine receptors in rat brain. Nature 275, 553–555 (1978). https://doi.org/10.1038/275553a0

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