A novel allosteric modulatory site on the GABAA receptor β subunit
作者： K.A. Wafford , C.J. Bain , K. Quirk , R.M. McKernan , P.B. Wingrove
DOI: 10.1016/0896-6273(94)90330-1
关键词:
摘要: Abstract Cloning of cDNAs that code for GABA A receptor subunits has revealed multiple populations constructed from different subunit combinations. On native rat and cloned human receptors, the anticonvulsant compound loreclezole strongly potentiated GABA-mediated chloride currents. Using combinations expressed in Xenopus oocytes transfected 293 cells, was highly selective receptors containing β2 or β3 over those β1 subunit. Loreclezole demonstrated to act at a site distinct benzodiazepine, barbiturate, steroid sites with unique dependence. These results describe previously unidentified modulatory on β allows pharmacological discrimination subpopulations brain provides new target putative anticonvulsant/anxiolytic drugs.
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