Functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit
S A Thompson1, T P Bonnert, P J Whiting
1Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Harlow, Essex, UK.
Abstract:
(1) This paper further examines the functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit expressed in Xenopus oocytes. (2) Alpha1beta1epsilon receptors are not modulated by benzodiazepine ligands or by a number of hypothalamic hormones. (3) The intravenous anaesthetic agents pentobarbital, propofol and etomidate all potentiate sub-maximal GABA currents (EC20) to a similar degree in alpha1beta1epsilon and alpha1beta1gamma2s receptors. (4) Direct activation by pentobarbital produced a similar maximum response on alpha1beta1epsilon and alpha1beta1gamma2s, however, both the EC50 and slope were lower on alpha1beta1epsilon compared to alpha1beta1gamma2s. (5) These results describe a novel pharmacology for recombinant alpha1beta1epsilon receptors.
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