TABLE 1

Dose-response curves for current stimulation by diazepam

Cumulative concentration-response curves were carried out at different GABA concentrations. The diazepam concentrations were 1, 10, 100, and 1000 nM. Stimulation went through an optimum. At 10,000 nM, stimulation was less than at 1000 nM. Data are given as means ± S.D. from four experiments each.

Subunit Combination GABA Diazepam Ka Diazepam Emax
μM nM %
α1 - β2 - α12 - β2 5 75 ± 15 255 ± 51
α1 - β2 - α12 - β2Y205S 15 87 ± 20 163 ± 22
α1 - β2 - α12 - β2Y205S 30 87 ± 23 157 ± 24
α1 - β2Y205S - α12 - β2 15 47 ± 14 142 ± 28
α1 - β2Y205S - α12 - β2 30 72 ± 10 106 ± 13
α1 - β2Y205S - α12 - β2 60 68 ± 19 70 ± 9