Evidence for inhibitory effect of the agonist gaboxadol at human alpha(1)beta(2)gamma S-2 GABA(A) receptors
Gaboxadol (THIP; 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) is an agonist at GABA(A) receptors. THIP concentrations (0.01-50 mM) were applied rapidly to Sf9 cells expressing the human alpha(1)beta(2)gamma(2S) GABA(A) receptors. The EC50 values for the peak current in THIP alone or THIP plus 1 muM diazepam were 154 and 53 muM, respectively. In supersaturating THIP (10-50 mM) the rate of curren