Membrane potential-dependent inhibition of the Na+,K+-ATPase by para-nitrobenzyltriethylammonium bromide.

ABSTRACT: Membrane potential (V(M))-dependent inhibitors of the Na(+),K(+)-ATPase are a new class of compounds that may have inherent advantages over currently available drugs targeting this enzyme. However, two questions remain unanswered regarding these inhibitors: (1) what is the mechanism of V(M)-dependent Na(+),K(+)-ATPase inhibition, and (2) is their binding affinity high enough to consider them as possible lead compounds? To address these questions, we investigated how a recently synthesized V(M)-dependent Na(+),K(+)-ATPase inhibitor, para-nitrobenzyltriethylamine (pNBTEA), binds to the enzyme by measuring the extracellular pNBTEA concentration and V(M) dependence of ouabain-sensitive transient charge movements in whole-cell patch-clamped rat cardiac ventricular myocytes. By analyzing the kin

SUBMITTER: Peluffo RD 

PROVIDER: S-EPMC3382828 | biostudies-literature | 2012 Jul

REPOSITORIES: biostudies-literature