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However, the <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2 receptor possessed significantly lower GABA efficacy compared with the <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L receptor. While the <jats:italic>\u03b3<\/jats:italic>2\u2010subunit was essential to the potency of GABA, its influence on the apparent GABA\u2010site antagonism was less profound. The antagonist affinity constants (<jats:italic>K<\/jats:italic><jats:sub>B<\/jats:sub>) of bicuculline inhibition and slopes of Schild plots were similar between all types of ternary and binary receptors except <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2 receptor which was not tested. The p<jats:italic>K<\/jats:italic><jats:sub>B<\/jats:sub>s and IC<jats:sub>50<\/jats:sub>s of the GABA\u2010site antagonism were not significantly different between the <jats:italic>\u03b1<\/jats:italic>1<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L, <jats:italic>\u03b1<\/jats:italic>4<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L and <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L receptors. Bicuculline blocked pentobarbital\u2010activated currents in a reversible and non\u2010competitive manner with the <jats:italic>\u03b1<\/jats:italic>1<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L, <jats:italic>\u03b1<\/jats:italic>4<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L, and <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L receptors, indicating an allosteric inhibition of the GABA\u2010site. No significant difference of bicuculline potencies in inhibiting GABA\u2010 and pentobarbital\u2010activated currents was found between the <jats:italic>\u03b1<\/jats:italic>1<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L, <jats:italic>\u03b1<\/jats:italic>4<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L and <jats:italic>\u03b1<\/jats:italic>5<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L receptors.<\/jats:p><jats:p><jats:bold>Conclusion:\u2002<\/jats:bold> The GABA\u2010site antagonism does not depend on the subtype of <jats:italic>\u03b1<\/jats:italic>\u2010subunits. Similarly, pentobarbital activates ternary receptors composed of different <jats:italic>\u03b1<\/jats:italic>\u2010subunits in a bicuculline\u2010sensitive manner. The potencies of bicuculline to inhibit pentobarbital\u2010activated currents are identical with receptors containing <jats:italic>\u03b1<\/jats:italic>1, <jats:italic>\u03b1<\/jats:italic>4 or <jats:italic>\u03b1<\/jats:italic>5\u2010subunit. The <jats:italic>\u03b1<\/jats:italic>1<jats:italic>\u03b2<\/jats:italic>2 and <jats:italic>\u03b1<\/jats:italic>4<jats:italic>\u03b2<\/jats:italic>2 receptors possess higher GABA potencies compared with the <jats:italic>\u03b1<\/jats:italic>1<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L and <jats:italic>\u03b1<\/jats:italic>4<jats:italic>\u03b2<\/jats:italic>2<jats:italic>\u03b3<\/jats:italic>2L receptors.<\/jats:p>","DOI":"10.1111\/j.1748-1716.2006.01593.x","type":"journal-article","created":{"date-parts":[[2006,5,25]],"date-time":"2006-05-25T09:25:14Z","timestamp":1148549114000},"page":"479-488","source":"Crossref","is-referenced-by-count":11,"title":["GABA\u2010site antagonism and pentobarbital actions do not depend on the <i>\u03b1<\/i>\u2010subunit type in the recombinant rat GABA<sub>A<\/sub> 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