Receptor Subtype | RY-80 | RY-24 | Flunitrazepam |
---|---|---|---|
α5β3γ2 | 70 ± 6 | 75 ± 2 | 168 ± 14 |
α5I215V β3γ2 | 91 ± 7 | 94 ± 6 | 154 ± 5 |
α5I215T β3γ2 | 97 ± 7 | 102 ± 7 | 167 ± 5 |
α5I215K β3γ2 | 62 ± 4 | 73 ± 4 | 169 ± 18 |
Wild-type or mutant GABAA receptors were expressed in X. laevis oocytes and electrophysiological recordings were performed as described under Materials and Methods. Responses to concentrations of GABA in presence of drugs are reported as a percentage of the response to GABA alone (% control). GABA was applied at concentration 30 μM, approximating its EC50 value at each receptor subtype tested (EC50 = 25.8 ± 7.8 μM). RY-80, RY-24, and flunitrazepam were used at a saturating concentration of 1 μM. Values are means ± S.D. for at least three oocytes.