Add time:07/30/2019         Source:sciencedirect.com

Publisher SummaryThe neutral amino acid γ-aminobutyric acid (GABA) is an inhibitory neurotransmitter in the central nervous system (CNS) and is involved as a transmitter or a paracrine effector in the regulation of a variety of physiological mechanisms in the periphery. The most flexible approaches to stimulation of GABA neurotransmission processes appear to be facilitation of the effect of synaptically released GABA via GABA receptor modulatory sites or by interfering with the inactivation of GABA. The most logical strategies for pharmacological interventions with the purpose of stimulating GABA neurotransmission are (1) effective blockade of neuronal and glial GABA uptake for enhancing the inhibitory effects of synaptically released GABA or (2) selective blockade of glial GABA uptake to increase the amount of GABA taken up into the nerve terminals. Selective neuronal GABA transport inhibitors might conceivably produce convulsions as the result of the depletion of GABA from nerve terminals; earlier animal behavioral studies have demonstrated that neuronal GABA transport inhibitors/substrates produce convulsions, whereas selective inhibitors of glial GABA transport show anticonvulsant effects.

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