Table 1.

Apparent affinites of wild-type and mutant receptors for GABA, SR-95531, and pentobarbital

ReceptorGABASR-95531PB
EC50m)nHnwt/mutKim)nwt/mutEC50m)nwt/mut
α1β2 Wild type4.3  ± 1.21.181.00.12  ± 0.0281.0570  ± 6651.0
α1β2-V199C3.1  ± 0.41.440.70.08  ± 0.0130.6577  ± 19551.0
α1β2-F200C1292  ± 170*1.143004.34  ± 2.6*336.2712  ± 9631.2
α1β2-S201C725  ± 160*0.5*41701.42  ± 0.3*311.81038  ± 42531.8
α1β2-T202C61100  ± 10900*1.05140001.90  ± 0.4*315.8690  ± 17031.2
α1β2-G203C20480  ± 6990*1.01048004.67  ± 0.4*438.91088  ± 7031.9
α1β2-S204C1.5  ± 0.31.160.30.05  ± 0.0350.4427  ± 8650.7
α1β2Y205C78000  ± 7070*1.451800012.40  ± 1.5*3103.3800  ± 4241.4
α1β2-P206C2.6  ± 1.01.240.60.53  ± 0.1364.4347  ± 4640.6
α1β2-R207C310  ± 30*1.34700.11  ± 0.0240.9480  ± 7240.8
α1β2-L208C2.7  ± 0.51.550.60.07  ± 0.0230.6327  ± 7750.6
α1β2-S209C5.4  ± 1.11.131.30.11  ± 0.0130.9583  ± 10531.0
  • EC50 and Ki values are presented as mean ± SEM. An asterisk indicates that the value is significantly different from wild type (p < 0.01). PB, Pentobarbital; wt, wild type; mut, mutant.