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Intracellular Regulation of GABAA-Receptor Function

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Ion Channels

Part of the book series: Ion Channels ((IC))

Abstract

γ-Aminobutyric acid (GABA) was reported to occur in brain tissue in 1950 in three studies (Awapara et al., 1950; Roberts and Frankel, 1950; Udenfriend, 1950). A long and often controversial discussion about the function of GABA (for review see Roberts, 1986) followed. Physiological effects of GABA were first studied at the crustacean neuromuscular junction (for review see Takeuchi, 1976 Kravitz et al., 1968). The role of GABA as inhibitory transmitter in the mammalian CNS was established in 1967 through electrophysiological studies comparing the properties of evoked inhibitory postsynaptic potentials with responses to iontophoretically applied GABA: GABA-induced hyperpolarization was accompanied by a large increase in membrane conductance (Krnjevic and Schwartz, 1967). It is now widely accepted that GABA is the main transmitter of synaptic inhibition in the mammalian CNS. The notion of a transmitter function of GABA has been corroborated by a variety of studies: the GABA-synthesizing enzyme glutamate decarboxylase (L-glutamate-1carboxylase, EC 4.1.1.15) is concentrated in nerve terminals of GABAergic neurons (Salganicoff and De Robertis, 1965; Fonnum, 1968; Fonnum and Walberg, 1973; Saito et al., 1974). GABA is released from brain tissue upon stimulation by a Ca2+-dependent mechanism (Srinivasan et al., 1969; Obata and Takeda, 1969; Iversen et al., 1971; Roberts, 1974) and is eliminated from extracellular spaces by a Na+-dependent uptake into nerve cells or glial cells (Iversen and Neal, 1968; Henn and Hamberger, 1971; Bloom and Iversen, 1971; Schrier and Thompson,1974).

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  1. Department of Pharmacology, State University of New York, Brooklyn, New York, 11203, USA

    Armin Stelzer

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  1. Northwestern University Medical School, Chicago, Illinois, USA

    Toshio Narahashi

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Stelzer, A. (1992). Intracellular Regulation of GABAA-Receptor Function. In: Narahashi, T. (eds) Ion Channels. Ion Channels. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3328-3_4

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