Abstract
Characteristics of 3H-GABA binding to rat brain synaptic membranes in vitro have been investigated. The specific binding of 3H-GABA displays saturation kinetics. Only one single population of receptor sites was found (K m=31.3 nM) with a concentration of 2.09 pmol/mg protein. Only GABA agonists show inhibitory effect on the binding, whereas GABA antagonists, GABA-uptake inhibitors, and inhibitors of GAD and GABA-T are without effect. The order of potencies for GABA agonists are: Muscimol > GABA ≥ 4,5-dihydromuscimol > 3-aminopropane sulphonic acid > isoguvacine > THIP > 3-hydroxy-GABA > imidazol-4-acetic acid. Agonists and antagonists from other neurone systems as well as neuroleptics and benzodiazepines had no or only a very slight potency in the binding test.
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Hyttel, J. Characterization of 3H-GABA receptor binding to rat brain synaptosomal membranes: Effect of non GABAergic compounds. Psychopharmacology 65, 211–214 (1979). https://doi.org/10.1007/BF00433051
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DOI: https://doi.org/10.1007/BF00433051