α Subunit isoform influences GABAA receptor modulation by propofol

Add time:07/25/2019    Source:sciencedirect.com

We have investigated the role of the α subunit in the modulation of γ-aminobutyric acid type A (GABAA) receptors by the general anesthetic propofol, using whole-cell patch clamp recordings made from distinct stable fibroblast cell lines which expressed only α1β3γ2 or α6β3γ2 GABAA receptors. At clinically relevant anesthetic concentrations, propofol potentiated submaximal GABA currents in α1β3γ2 receptors to a far greater degree than those in α6β3γ2 receptors. The a subunit influenced the efficacy of propofol for modulation, but not its potency. In contrast, direct gating of the ion channel by propofol, in the absence of GABA, was significantly larger in the α6 than the α1 containing receptors. The potentiation of submaximal GABA by trichloroethanol, and the potentiation and direct gating by methohexital was also studied, and showed the same relative trends as propofol.

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