GSK 1702934A

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Cardiovascular Disease

TRPC3

GSK1702934A is able to induce TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6 with an EC50 of 0.08 mM and 0.44 mM, respectively[1]. GSK1702934A induces a transient, non-selective conductance and prolonged action potentials in TRPC3-overexpressing myocytes but not in wild-type myocytes[2]. GSK1702934A substantially promotes NCX currents in TRPC3-overexpressing myocytes[2].

[1]. de la Cruz GG, et al. Intensified Microwave-Assisted N-Acylation Procedure - Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core. Synlett. 2017 Apr;28(6):695-700.

[2]. Doleschal B, et al. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73.