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Rosiglitazone inhibits vascular KATP channels and coronary vasodilation produced by isoprenaline

Lei Yu1, Xin Jin, Yang Yang

  • 1Department of Biology, Georgia State University, Atlanta, GA 30302, USA.

British Journal of Pharmacology
|June 16, 2011
PubMed
Abstract

Insights

Rosiglitazone, an anti-diabetic drug, inhibits vascular ATP-sensitive potassium (KATP) channels. This action impairs coronary circulation regulation and may explain cardiovascular risks associated with this medication.

Area of Science:

  • Cardiovascular Pharmacology
  • Molecular Cardiology
  • Endocrinology

Background:

  • Rosiglitazone is an anti-diabetic medication.
  • Clinical trials have yielded conflicting results regarding rosiglitazone's cardiovascular safety.
  • Understanding rosiglitazone's vascular effects is crucial.

Purpose of the Study:

  • Investigate rosiglitazone's impact on coronary circulation.
  • Identify potential vascular targets of rosiglitazone.
  • Elucidate the mechanism behind rosiglitazone's cardiovascular effects.

Main Methods:

  • Expressed K(IR) 6.1/SUR2B channels in HEK293 cells for patch-clamp studies.
  • Utilized Langendorff heart preparation in wild-type and K(IR) 6.1-null mice.
  • Assessed coronary vasodilation and perfusion in response to rosiglitazone.

Main Results:

  • Rosiglitazone inhibited K(IR) 6.1/SUR2B channels in a membrane-delimited manner.
  • Glibenclamide enhanced rosiglitazone's inhibitory effect, with an IC(50) of 2µM.
  • Rosiglitazone concentration-dependently inhibited isoprenaline-induced coronary vasodilation in wild-type mice.
  • This effect was significantly attenuated in K(IR) 6.1-null mice.

Conclusions:

  • The vascular K(ATP) channel is a direct target of rosiglitazone.
  • Rosiglitazone's inhibition of vascular K(ATP) channels may compromise coronary circulation.
  • This mechanism could contribute to cardiovascular risks observed with rosiglitazone therapy.

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