UK-59811 HYDROCHLORIDE

Descriptions

Biochem/physiol Actions

UK-59811 is a 1,4-dihydropyridine calcium channel blocker. It has been used in a crystallographic and functional analysis of drug binding to the bacterial homotetrameric model voltage-gated calcium channel CaVAb, comparing 1,4-dihydropyridine binding to phenylalkylamine binding. UK-59811 inhibited CaVAb with an IC50 value of 194 nM, binding at the outer, lipid-facing surface of the pore at the interface between two CaVAb subunits, while at concentrations above 1 µM, it also bound in the pore. It was contrasted with phenylalkylamine Br-verapamil which binds on the intracellular side of the selectivity filter in the central cavity of the pore, physically blocking the pore.

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