Table 2.

Binding affinities of Ro15-1788, flurazepam, zolpidem, and DMCM for wild-type (α 1β 2γ 2) and mutant receptors

ReceptorRo15–1788FlurazepamZolpidemDMCM
KinKinKinKin
αβγ5.1 ± 1.53165 ± 235108 ± 22310.8 ± 2.43
αβγW183C4.6 ± 0.43117 ± 73213 ± 5735.5 ± 0.63
αβγE189C7.7 ± 2.43213 ± 403198 ± 10416.8 ± 3.53
αβγR197C5.1 ± 1.0468 ± 12*347 ± 7320.4 ± 5.53
  • Ki values were determined by displacement of [3H] Ro15-1788 binding and represent the equilibrium dissociation constant (apparent affinity) of the unlabeled ligand. Data represent mean ± SD for n experiments. Values significantly different from WT receptors are indicated (*p < 0.05).