Figure 9. Effect of mutations of α1 R84P, M89L and I120L on efavirenz sensitivity in α1β2γ2 GABAA receptors.
A, Representative traces showing EC30 GABA currents with or without co-application of efavirenz (10 or 30 μM) in wild type, α1(R84P/M89L)β2γ2 and α1(R84P/M89L/I120L)β2γ2 receptors. B, Summary data for efavirenz effect on wild type and mutant α1β2γ2 GABAA receptors. Minimum of five cells were tested for efavirenz. Note that efavirenz-mediated potentiation was completely lost in all mutant receptors. p>0.05, paired t-test, compared to control; p<0.05, unpaired t-test, compared to wild type.