Table 2

Ki values for zopiclone and diazepam binding at GABAA receptors containing wild-type and mutant α-subunits

α-Subunits[3H]Ro15-4513 (Kd)Zopiclone (Ki)Times Wild TypeDiazepam (Ki)Times Wild Type
nM nM
Wild type6.2  ± 0.542-a 51.3  ± 5.419.4  ± 0.3
H101F0.95  ± 0.072-a 199  ± 284164  ± 498
H101Y7.01  ± 0.712-a 863  ± 38917504  ± 5125
H101Q0.49  ± 0.072-a 761  ± 216151476  ± 78274
H101E2.13  ± 0.132-a >10,000>10,000
H101K1.54  ± 0.112-a >10,000>10,000
H101A8.3  ± 0.4>10,000>10,000

Values are means ± S.E. for at least three experiments performed in duplicate.

    • 2-a  Values reported previously (Davies et al., 1998).