GSK1702934A is an activator of transient receptor potential canonical 3 (TRPC3) and TRPC6.1 It induces TRPC3- and TRPC6-dependent currents in whole-cell patch-clamp assays using HEK293 cells expressing the human channels (EC50s = 0.08 and 0.44 ?M, respectively). GSK1702934A enhances contractility and induces arrhythmias in hearts isolated from TRPC3-overexpressing, but not wild-type, mice.2
1.Xu, X., Lozinskaya, I., Costell, M., et al.Characterization of small molecule TRPC3 and TRPC6 agonist and antagonistsBiophys. J.104(2)454A(2013) 2.Doleschal, B., Primessnig, U., W?lkart, G., et al.TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1Cardiovasc. Res.106(1)163-173(2015)