The Journal of pharmacology and experimental therapeutics
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J. Pharmacol. Exp. Ther. · Aug 1995
Modulation of the GABAA receptor by propofol is independent of the gamma subunit.
Many anxiolytics, anticonvulsants and general anesthetics modulate gamma-aminobutyric acid type A (GABAA) receptors. The anxiolytic benzodiazepines potentiate the actions of GABA, and this only at GABAA receptors with gamma subunits. The general anesthetics both potentiate GABA and activate GABAA receptors directly, but their binding sites on the receptor are poorly defined. ⋯ In addition to activating currents directly, propofol potentiated currents elicited by GABA recorded from cells expressing either subunit combination. We conclude that the gamma 2 subunit is not a prerequisite for activation of GABAA receptors by propofol or for its potentiation of GABA-activated currents. However, the subunit may contribute to the efficacy of propofol as a GABAA receptor activator.