Figure 5.
Concentration-response relationships for direct activation of α1(L264T)β3γ2L and α1(L264T)β1γ2L γ-aminobutyric acid type A receptors by R-etomidate (A), S-etomidate (B), cyclopropyl etomidate (C), and dihydrogen etomidate (D). Data obtained from oocytes expressing α1(L264T)β3γ2L and α1(L264T)β1γ2L γ-aminobutyric acid type A receptors are labeled as β3 and β1, respectively. Each directly activated peak current amplitude was normalized to the peak current elicited by 100 μM γ-aminobutyric acid in the same oocyte. Each data point represents the average normalized amplitude (± SD) obtained from 6 separate oocytes. The curves are fits of the data sets to a Hill equation in the form: Y=100/(1+[EC50/X]Hill coefficient), where EC50 is a drug’s half-maximal direct activating concentration. In the case of cyclopropyl etomidate, the 1000 μM data points were not included in the fits. For all drugs, the EC50 for direct activation was significantly lower in α1(L264T)β3γ2L than α1(L264T)β1γ2L γ-aminobutyric acid type A receptors.