Cardioselectivity of the sulphonylurea HMR 1098: studies on native and recombinant cardiac and pancreatic K(ATP) channels.

ABSTRACT: In this study we investigated the effects of the putative cardioselective sulphonylurea derivative HMR 1098 on ATP-sensitive potassium (K(ATP)) channels from cardiac ventricular myocytes, the INS-1 beta-cell line and from recombinant K(ATP) channels composed of SUR2A/Kir6.2, SUR1/Kir6.2, SUR1/Kir6.1 an Kir6.2,DeltaC26. Recombinant channels were expressed in tsA201 or COS-1 cells. The effects of HMR 1098 on single channel and whole-cell currents were recorded using the patch-clamp technique. At the single channel level, using excised inside-out membrane patches, HMR 1098 inhibited K(ATP) channels from ventricular cells and INS-1 cells with IC(50)s of 0.88 and 720 microM respectively. Similar results to those in cardiac cells were obtained using recombinant SUR2A/Kir6.2 K(ATP) channels. HMR

SUBMITTER: Manning Fox JE 

PROVIDER: S-EPMC1573135 | biostudies-literature | 2002 Jan

REPOSITORIES: biostudies-literature