Wiener klinische Wochenschrift
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GABAA-benzodiazepine receptors and epilepsy. gamma-Aminobutyric acid (GABA) is quantitatively one of the most important neurotransmitters in the central nervous system. Since the predominant action of GABA on neurons is inhibitory, activation of GABA receptors, and especially of GABAA receptors, causes an anticonvulsive effect. GABAA receptors can be activated either directly by GABA or GABA-agonists, or indirectly by allosteric modulation of these receptors. ⋯ These compounds cause convulsions and are called "inverse agonists" of the benzodiazepine receptors. Recent evidence indicates the existence of several different benzodiazepine receptor (and, thus, GABAA receptor) subtypes. Since these receptor subtypes exhibit a different regional distribution in the central nervous system, the development of subtype-selective GABAA receptor agonists or benzodiazepine receptor agonists should result in anticonvulsants with less side effects.