Selective activation of Ca2+ -dependent K+ channels by novel benzimidazolone

摘要: Activators and blockers of specific ion channels are important pharmacological tools for characterizing their influence on cell function. The large-conductance Ca(2+)-dependent K+ channel (BK channel) is blocked by peptides such as charybdotoxin iberiotoxin, but no selective activator the has been described. Here we report single-channel whole-cell patch-clamp experiments activation BK in aortic smooth muscle cells with a new heterocyclic molecule, NS 1619 (1-(2'-hydroxy-5'-trifluoromethylphenyl)-5-trifluoromethyl- 2(3H)benzimidazolone). effect was dose-dependent, resulting shift curve up to -50 mV towards negative membrane potentials. fully reversible antagonized well tetraethylammonium ions. compound hyperpolarized cells. type activator, which may significantly modulate excitability.