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α Subunit isoform influences GABA A receptor modulation by propofol
Journal article   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

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Abstract

We have investigated the role of the alpha subunit in the modulation of gamma-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 alpha1beta3gamma2 or alpha6beta3gamma2 GABA(A) receptors. At clinically relevant anesthetic concentrations, propofol potentiated submaximal GABA currents in alpha1beta3gamma2 receptors to a far greater degree than those in alpha6beta3gamma2 receptors. The alpha 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 alpha6 than the alpha1 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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