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Description

A cell permeable hydroxytricyclic derivative that acts as a specific and reversible inhibitor of transient receptor potential melastatin 4 (TRPM4) (IC50 = 20 µ,M in HEK293 cells). Does not affect TRPM5 and cystic fibrosis transmembrane conductance regulators (CFTR) channels. Decreases the occurrence of early after depolarizations (EAD) and exhibits an anti-arrhythmic effect that is independent of the action of protein kinase A. Shown to abolish NMDA-induced burst firing in dopaminergic neurons. Does not affect K+ currents at ~10 µ,M, but at higher concentration (~100 µ,M) it reversibly reduces K+ currents.