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α Subunit isoform influences GABA A receptor modulation by propofol
Journal article   Open access   Peer reviewed

α Subunit isoform influences GABA A receptor modulation by propofol

M.D Krasowski, S.M O'Shea, C.E.M Rick, P.J Whiting, K.L Hadingham, C Czajkowski and N.L Harrison
Neuropharmacology, Vol.36(7), pp.941-949
1997
DOI: 10.1016/S0028-3908(97)00074-9
PMID: 9257938
url
https://www.ncbi.nlm.nih.gov/pmc/articles/2857729View
Open Access

Abstract

We have investigated the role of the α subunit in the modulation of γ-aminobutyric acid type A (GABA A) receptors by the general anesthetic propofol, using whole-cell patch clamp recordings made from distinct stable fibroblast cell lines which expressed only α 1 β 3 γ 2 or α 6 β 3 γ 2 GABA A receptors. At clinically relevant anesthetic concentrations, propofol potentiated submaximal GABA currents in α 1 β 3 γ 2 receptors to a far greater degree than those in α 6 β 3 γ 2 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 α 6 than the α 1 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.
GABA trichloroethanol GABA A receptor methohexital propofol anesthesia

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