Activation of GPER increased peak INa but had no
effect on INaL and INa kinetics
To further investigate whether the effect of estrogen is mediated by
GPER, hiPSC-CMs were treated with GPER
agonists (G1, 11 nmol/L) and
antagonists (G15, 20 nmol/L) for
30 min. Activation and inhibition of GPER did not affectI NaL in hiPSC-CMs (Figure 5A and C). G1 increased
peak I Na density similar to E2, and the effects
of E2 were eliminated by G15 which indicates that GPER mediated the
effect of estrogen on peak I Na (Figure 5B, D and
E). GPER did not affect the V1/2 and k values of
activation and inactivation (Figure 5F and H-K). Interestingly,
treatment with G15 alone increased the τ value of recovery from
inactivation (Figure 5G and L; Supplemental Figure 3A). Data values for
these results are provided in supplementary material online,
Supplemental Table 1-7.