Abstract
A STEREOSPECIFIC, saturable, high affinity binding site for 3H-diazepam has recently been characterised in membrane fractions isolated from the brains of mammals1, including man2, which has been suggested to represent the pharmacological benzodiazepine (BZ) receptor2–4. Electrophysiological5 and biochemical6 results indicate that BZs exert their main actions in the central nervous system by facilitation of the synaptic action of γ-aminobutyric acid (GABA). Evidence for an interaction between GABA and BZs at the receptor level has recently been obtained7–11. Thus, GABA has been shown to stimulate BZ binding8–11 and there is preliminary evidence that this process is mediated by a specific GABA recognition site, as the GABA agonists muscimol8, imidazoleacetic acid11, and 3-guanidino-propionic acid11 also stimulate 3H-diazepam binding. We now report different structural requirements for stimulation of 3H-diazepam binding to rat brain synaptic membranes compared with those for inhibition of Na+-independent 3H-GABA binding12. We suggest that stimulation by GABA of BZ receptor binding involves a novel type of a GABA receptor.
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KAROBATH, M., PLACHETA, P., LIPPITSCH, M. et al. Is stimulation of benzodiazepine receptor binding mediated by a novel GABA receptor?. Nature 278, 748–749 (1979). https://doi.org/10.1038/278748a0
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DOI: https://doi.org/10.1038/278748a0
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