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Research ArticleMinireview—A Latin American Perspective on Ion Channels

Pharmacological Conversion of a Cardiac Inward Rectifier into an Outward Rectifier Potassium Channel

Eloy G. Moreno-Galindo, Jose A. Sanchez-Chapula, Martin Tristani-Firouzi and Ricardo A. Navarro-Polanco
Molecular Pharmacology September 2016, 90 (3) 334-340; DOI: https://doi.org/10.1124/mol.116.104950
Eloy G. Moreno-Galindo
Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Colima, México (E.G.M.-G., J.A.S.-C., R.A.N.-P.); Nora Eccles Harrison Cardiovascular Research and Training Institute, and Division of Pediatric Cardiology, University of Utah, Salt Lake City, Utah (M.T.-F.)
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Jose A. Sanchez-Chapula
Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Colima, México (E.G.M.-G., J.A.S.-C., R.A.N.-P.); Nora Eccles Harrison Cardiovascular Research and Training Institute, and Division of Pediatric Cardiology, University of Utah, Salt Lake City, Utah (M.T.-F.)
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Martin Tristani-Firouzi
Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Colima, México (E.G.M.-G., J.A.S.-C., R.A.N.-P.); Nora Eccles Harrison Cardiovascular Research and Training Institute, and Division of Pediatric Cardiology, University of Utah, Salt Lake City, Utah (M.T.-F.)
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Ricardo A. Navarro-Polanco
Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, Colima, México (E.G.M.-G., J.A.S.-C., R.A.N.-P.); Nora Eccles Harrison Cardiovascular Research and Training Institute, and Division of Pediatric Cardiology, University of Utah, Salt Lake City, Utah (M.T.-F.)
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Abstract

Potassium (K+) channels are crucial for determining the shape, duration, and frequency of action-potential firing in excitable cells. Broadly speaking, K+ channels can be classified based on whether their macroscopic current outwardly or inwardly rectifies, whereby rectification refers to a change in conductance with voltage. Outwardly rectifying K+ channels conduct greater current at depolarized membrane potentials, whereas inward rectifier channels conduct greater current at hyperpolarized membrane potentials. Under most circumstances, outward currents through inwardly rectifying K+ channels are reduced at more depolarized potentials. However, the acetylcholine-gated K+ channel (KACh) conducts current that inwardly rectifies when activated by some ligands (such as acetylcholine), and yet conducts current that outwardly rectifies when activated by other ligands (for example, pilocarpine and choline). The perplexing and paradoxical behavior of KACh channels is due to the intrinsic voltage sensitivity of the receptor that activates KACh channels, the M2 muscarinic receptor (M2R). Emerging evidence reveals that the affinity of M2R for distinct ligands varies in a voltage-dependent and ligand-specific manner. These intrinsic receptor properties determine whether current conducted by KACh channels inwardly or outwardly rectifies. This review summarizes the most recent concepts regarding the intrinsic voltage sensitivity of muscarinic receptors and the consequences of this intriguing behavior on cardiac physiology and pharmacology of KACh channels.

Footnotes

    • Received April 27, 2016.
    • Accepted May 27, 2016.
  • This study was supported by SEP-CONACYT, México [Grants CB-2011-01-167109 to E.G.M.-G., CB-2013-01-220546 to J.A.S.-C., and CB-2013-01-220742 to R.A.N.-P.]

  • dx.doi.org/10.1124/mol.116.104950.

  • Copyright © 2016 by The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 90 (3)
Molecular Pharmacology
Vol. 90, Issue 3
1 Sep 2016
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Research ArticleMinireview—A Latin American Perspective on Ion Channels

Conversion of an Inward into an Outward Rectifier Channel

Eloy G. Moreno-Galindo, Jose A. Sanchez-Chapula, Martin Tristani-Firouzi and Ricardo A. Navarro-Polanco
Molecular Pharmacology September 1, 2016, 90 (3) 334-340; DOI: https://doi.org/10.1124/mol.116.104950

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Research ArticleMinireview—A Latin American Perspective on Ion Channels

Conversion of an Inward into an Outward Rectifier Channel

Eloy G. Moreno-Galindo, Jose A. Sanchez-Chapula, Martin Tristani-Firouzi and Ricardo A. Navarro-Polanco
Molecular Pharmacology September 1, 2016, 90 (3) 334-340; DOI: https://doi.org/10.1124/mol.116.104950
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  • Article
    • Visual Overview
    • Abstract
    • Introduction
    • The Molecular Basis for Inward Rectification of Kir Channels
    • The Muscarinic G-Protein–Coupled Inward Rectifier KACh Channel
    • An Outward Rectifier K+ Current Activated by Muscarinic Ligands
    • Muscarinic Receptors Possess Intrinsic Voltage Sensitivity
    • The Mechanism for Pharmacological Conversion of an Inward Rectifier into an Apparent Delayed Rectifier K+ Channel
    • The Effect of Voltage on the Affinity and Efficacy of the M2R-Agonist Interaction
    • Physiologic Implications of M2R Voltage Sensitivity for Parasympathetic Regulation of the Heart
    • Conclusions
    • Acknowledgments
    • Authorship Contributions
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