GABA antagonists differentiate between recombinant GABAA/benzodiazepine receptor subtypes

摘要: Seventeen rat GABAA receptor subtypes were transiently expressed in the human embryonic kidney 293 cell line from alpha 1, 2, 3, 5, or 6 variants with any of three beta subunits and gamma 2S 3. We obtained fingerprints form subtype characteristic concentration-response curves 35S-TBPS binding to GABA antagonists SR 95531 bicuculline. 3 2S/3 5 containing receptors effectively recognized but not when was replaced by 1 2 subunit. This indicates a specific interaction high-affinity sites. At low levels allosterically increased all concentration magnitude depending on subunit combination. Exchange variant did alter for so receptors. displayed strong GABA-induced stimulation binding, whereas marginally increased. bicuculline decreased In addition, effective x threefold more potent than reversing modulation most types, 30-fold receptors.(ABSTRACT TRUNCATED AT 250 WORDS)