Block of human aorta Kir6.1 by the vascular KATP channel inhibitor U37883A

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S Surah-Narwal1, S Z Xu, D McHugh

  • 1School of Biomedical Sciences, Worsley Building, University of Leeds, Leeds, LS2 9JT, UK.

British Journal of Pharmacology
|October 12, 1999
PubMed

Insights

Human Kir6.1 (hKir6.1) is identified as a component of vascular ATP-sensitive potassium (KATP) channels. Its function with SUR1 suggests a molecular basis for distinguishing vascular KATP channel pharmacology.

Area of Science:

  • Molecular biology
  • Cardiovascular research
  • Ion channel physiology

Background:

  • ATP-sensitive potassium (KATP) channels are crucial in regulating vascular tone.
  • The specific subunits forming vascular KATP channels and their pharmacological properties remain incompletely understood.

Purpose of the Study:

  • To isolate and characterize a human homologue of the rat pancreatic Kir6.1 gene.
  • To investigate the functional role and pharmacological properties of the human Kir6.1 (hKir6.1) subunit in KATP channels.

Main Methods:

  • Screening a human aorta cDNA library to isolate hKir6.1.
  • Expressing hKir6.1 and SUR1 in Xenopus oocytes to study K+ channel activity.
  • Assessing the effects of KATP channel modulators (diazoxide, glibenclamide, U37883A) on expressed channels.

Main Results:

  • hKir6.1 was isolated and sequenced.
  • Co-expression of hKir6.1 and SUR1 in oocytes generated functional K+ channels activated by diazoxide and inhibited by glibenclamide.
  • hKir6.1+SUR1 channels showed sensitivity to the vascular-selective inhibitor U37883A, albeit with lower potency than native vascular tissues.

Conclusions:

  • hKir6.1 is a likely component of vascular KATP channels.
  • The pore-forming subunit (Kir6.1) influences KATP channel pharmacology, contributing to distinctions between vascular and other KATP channel types.
  • Additional factors may be involved in conferring the full pharmacological profile of native vascular KATP channels.

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