
Estrogen and SERMs rapidly attenuate the GABAB response. A-F, Representative traces of the GABAB responses before and after steroid treatment. Experiments were conducted as described in Figure 1. G, The chemical structures of E2 and the SERMs. H, Bar graphs summarizing the effects of E2 and SERMs on the baclofen response. E2 (100 nm) attenuated the GABAB receptor-mediated outward current by 41%. The inhibitory effects of E2 on the baclofen response were blocked by the estrogen receptor antagonist ICI 182,780 (1 μm). E2-BSA (100 nm), 4-OH tamoxifen (1 μm), raloxifene (1 μm), GW-5638 (1 μm), and STX (10 nm) also inhibited the baclofen response; however, 17α-E2 (1 μm) had no effect. Error bars represent the mean ± SEM of 4-11 cells tested per group. *p < 0.05, **p < 0.01, and ***p < 0.005, versus vehicle control group.




