Rosiglitazone selectively inhibits K(ATP) channels by acting on the K(IR) 6 subunit.

ABSTRACT:

Background and purpose

Rosiglitazone is an anti-diabetic drug acting as an insulin sensitizer. We recently found that rosiglitazone also inhibits the vascular isoform of ATP-sensitive K(+) channels and compromises vasodilatory effects of β-adrenoceptor activation and pinacidil. As its potency for the channel inhibition is in the micromolar range, rosiglitazone may be used as an effective K(ATP) channel inhibitor for research and therapeutic purposes. Therefore, we performed experiments to determine whether other isoforms of K(ATP) channels are also sensitive to rosiglitazone and what their sensitivities are.

Experimental approach

K(IR) 6.1/SUR2B, K(IR) 6.2/SUR1, K(IR) 6.2/SUR2A, K(IR) 6.2/SUR2B and K(IR) 6.2ΔC36 channels were expressed in HEK293 cells and were studied using

SUBMITTER: Yu L 

PROVIDER: S-EPMC3448911 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature