Functional characteristics of recombinant human GABA(A) receptors containing the epsilon-subunit.
(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.
Thompson
S A
SA
Neuroscience Research Centre, Merck Sharp & Dohme Research Laboratories, Harlow, Essex, UK.
Bonnert
T P
TP
Whiting
P J
PJ
Wafford
K A
KA
D018686:Anesthetics, Intravenous / Q000494:pharmacology; D000818:Animals; D001569:Benzodiazepines / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D009865:Oocytes / Q000378:metabolism; D012333:RNA, Messenger / Q000096:biosynthesis; D011963:Receptors, GABA-A / Q000737:chemistry* / Q000187:drug effects; D011994:Recombinant Proteins / Q000737:chemistry; D014982:Xenopus laevis
D018686:Anesthetics, Intravenous; D008024:Ligands; D012333:RNA, Messenger; D011963:Receptors, GABA-A; D011994:Recombinant Proteins; D001569:Benzodiazepines