W328M confers sensitivity to pentobarbital but not carisoprodol. A, in
wild-type homomeric ρ1 receptors, neither pentobarbital (300 μM) nor
carisoprodol (1 mM) enhanced GABA (EC20)-gated current. In W328M
mutant receptors, pentobarbital, but not carisoprodol, could enhance
GABA-activated currents. The GABA EC20 is denoted as control
current amplitude. B, similar phenomenon existed with regard to direct-gating
effects. In the W328M mutant receptors, pentobarbital could directly gate the
channel to approximately 15% of the maximal current amplitude gated by GABA.
In contrast, carisoprodol was ineffective in direct gating in either wild-type
or W328M mutant receptors. Each data point represents the mean ± S.E.
of four cells. Maximal GABA-gated current is denoted as 100%. *, significantly
different from the wild-type response (p < 0.05).