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Reviews in the Neurosciences

Editor-in-Chief: Huston, Joseph P.

Editorial Board: Topic, Bianca / Adeli, Hojjat / Buzsaki, Gyorgy / Crawley, Jacqueline / Crow, Tim / Gold, Paul / Holsboer, Florian / Korth, Carsten / Li, Jay-Shake / Lubec, Gert / McEwen, Bruce / Pan, Weihong / Pletnikov, Mikhail / Robbins, Trevor / Schnitzler, Alfons / Stevens, Charles / Steward, Oswald / Trojanowski, John

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Volume 22, Issue 3


Allosteric modulation of ATP-gated P2X receptor channels

Claudio Coddou
  • Section on Cellular Signaling, Program in Developmental Neuroscience, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD 20892-4510, USA
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/ Stanko S. Stojilkovic
  • Section on Cellular Signaling, Program in Developmental Neuroscience, National Institute of Child Health and Human Development, National Institutes of Health, Bethesda, MD 20892-4510, USA
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/ J. Pablo Huidobro-Toro
  • Centro de Envejecimiento y Regeneración, CARE, Centro Regulación Celular y Patología Prof. J.V. Luco, Instituto Milenio de Biología Fundamental y Aplicada, MIFAB, Departamento de Fisiología, Facultad de Ciencias Biológicas, P. Universidad Católica de Chile, Santiago, Chile
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Published Online: 2011-03-16 | DOI: https://doi.org/10.1515/rns.2011.014


Seven mammalian purinergic receptor subunits, denoted P2X1–P2X7, and several spliced forms of these subunits have been cloned. When heterologously expressed, these cDNAs encode ATP-gated non-selective cation channels organized as trimers. All activated receptors produce cell depolarization and promote Ca2+ influx through their pores and indirectly by activating voltage-gated calcium channels. However, the biophysical and pharmacological properties of these receptors differ considerably, and the majority of these subunits are also capable of forming heterotrimers with other members of the P2X receptor family, which confers further different properties. These channels have three ATP binding domains, presumably located between neighboring subunits, and occupancy of at least two binding sites is needed for their activation. In addition to the orthosteric binding sites for ATP, these receptors have additional allosteric sites that modulate the agonist action at receptors, including sites for trace metals, protons, neurosteroids, reactive oxygen species and phosphoinositides. The allosteric regulation of P2X receptors is frequently receptor-specific and could be a useful tool to identify P2X members in native tissues and their roles in signaling. The focus of this review is on common and receptor-specific allosteric modulation of P2X receptors and the molecular base accounting for allosteric binding sites.

Keywords: alcohol; allosterism; copper; neurosteroids; phosphoinositides; purinergic receptor channels; reactive oxygen species; zinc

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Published Online: 2011-03-16

Published in Print: 2011-06-01

Citation Information: Reviews in the Neurosciences, Volume 22, Issue 3, Pages 335–354, ISSN (Online) 2191-0200, ISSN (Print) 0334-1763, DOI: https://doi.org/10.1515/rns.2011.014.

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