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Molecular Pharmacology

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Research ArticleArticle

Hydrogen Sulfide as an Allosteric Modulator of ATP-Sensitive Potassium Channels in Colonic Inflammation

Aravind R. Gade, Minho Kang and Hamid I. Akbarali
Molecular Pharmacology January 2013, 83 (1) 294-306; DOI: https://doi.org/10.1124/mol.112.081596
Aravind R. Gade
Department of Pharmacology & Toxicology, Medical College of Virginia, VCU Program in Enteric Neuromuscular Sciences, Virginia Commonwealth University, Richmond, Virginia
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Minho Kang
Department of Pharmacology & Toxicology, Medical College of Virginia, VCU Program in Enteric Neuromuscular Sciences, Virginia Commonwealth University, Richmond, Virginia
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Hamid I. Akbarali
Department of Pharmacology & Toxicology, Medical College of Virginia, VCU Program in Enteric Neuromuscular Sciences, Virginia Commonwealth University, Richmond, Virginia
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Abstract

The ATP-sensitive potassium channel (KATP) in mouse colonic smooth muscle cell is a complex containing a pore-forming subunit (Kir6.1) and a sulfonylurea receptor subunit (SUR2B). These channels contribute to the cellular excitability of smooth muscle cells and hence regulate the motility patterns in the colon. Whole-cell voltage-clamp techniques were used to study the alterations in KATP channels in smooth muscle cells in experimental colitis. Colonic inflammation was induced in BALB/C mice after intracolonic administration of trinitrobenzene sulfonic acid. KATP currents were measured at a holding potential of −60 mV in high K+ external solution. The concentration response to levcromakalim (LEVC), a KATP channel opener, was significantly shifted to the left in the inflamed smooth-muscle cells. Both the potency and maximal currents induced by LEVC were enhanced in inflammation. The EC50 values in control were 6259 nM (n = 10) and 422 nM (n = 8) in inflamed colon, and the maximal currents were 9.9 ± 0.71 pA/pF (60 μM) in control and 39.7 ± 8.8 pA/pF (3 μM) after inflammation. As was seen with LEVC, the potency and efficacy of sodium hydrogen sulfide (NaHS) (10–1000 μM) on KATP currents were significantly greater in inflamed colon compared with controls. In control cells, pretreatment with 100 µM NaHS shifted the EC50 for LEV-induced currents from 2838 (n = 6) to 154 (n = 8) nM. Sulfhydration of sulfonylurea receptor 2B (SUR2B) was induced by NaHS and colonic inflammation. These data suggest that sulfhydration of SUR2B induces allosteric modulation of KATP currents in colonic inflammation.

Footnotes

  • This work was supported by the National Institutes of Health [Grant DK046367].

  • dx.doi.org/10.1124/mol.112.081596.

  • Received July 27, 2012.
  • Accepted October 31, 2012.
  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 83 (1)
Molecular Pharmacology
Vol. 83, Issue 1
1 Jan 2013
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Research ArticleArticle

Allosteric Modulation of KATP

Aravind R. Gade, Minho Kang and Hamid I. Akbarali
Molecular Pharmacology January 1, 2013, 83 (1) 294-306; DOI: https://doi.org/10.1124/mol.112.081596

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Research ArticleArticle

Allosteric Modulation of KATP

Aravind R. Gade, Minho Kang and Hamid I. Akbarali
Molecular Pharmacology January 1, 2013, 83 (1) 294-306; DOI: https://doi.org/10.1124/mol.112.081596
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