GABAA receptors: ligand-gated Cl- ion channels modulated by multiple drug-binding sites.
GABAA receptors are ligand-gated Cl- ion channels and the site of action of a variety of pharmacologically and clinically important drugs. In this review evidence is summarized indicating that these drugs, by interacting with several distinct binding sites at these receptors, allosterically modulate GABA-induced Cl- ion flux. Other results indicate that the affinity, as well as the modulatory efficacy of drugs, changes with receptor composition. A though investigation of the pharmacological properties of the individual binding sites on different GABAA receptor subtypes could open new avenues for selective modulation of GABAA receptors in different brain regions.
Sieghart
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Department of Biochemical Psychiatry, University Clinic for Psychiatry, Vienna, Austria.
D000818:Animals; D018118:Chloride Channels; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects*; D008024:Ligands; D008565:Membrane Proteins / Q000187:drug effects*; D011955:Receptors, Drug / Q000187:drug effects*; D011963:Receptors, GABA-A / Q000187:drug effects*
D018118:Chloride Channels; D008024:Ligands; D008565:Membrane Proteins; D011955:Receptors, Drug; D011963:Receptors, GABA-A