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Abstract

The simple amino acid GABA (γ-amin0butyric acid, 4-aminobutanoic acid) is a transmitter of major significance in the mammalian central nervous system. Receptors for GABA are found at both presynaptic (“axoaxonic7”) and postsynaptic (“axosomatic” and “axodendritic”) sites and also on nerve fibers (“nonsynaptic” or “fiber” receptors). There is strong evidence for a multi plicity of GABA receptors. Activation of GABA receptors may be studied in vivo using electrophysiological or behavioral methods and in vitro using isolated tissue preparations. Such studies of receptor activation are complemented by neurochemical investigation of the binding of GABA and related ligands to a variety of CNS membrane preparations. These studies provide direct information on the kinetics of binding interactions but only rather indirect information on the relevance of these interactions to physiological processes. Binding to the recognition sites on GABA receptors is merely the initial stage in producing the changes in ionic permeability that influence membrane potential and neuronal excitability. GABA agonist binding is considered to change receptor conformation with the activated receptor influencing an associated ionophore.

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Johnston, G.A.R., Allan, R.D., Skerritt, J.H. (1984). GABA Receptors. In: Lajtha, A. (eds) Handbook of Neurochemistry. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-4568-8_8

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