IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F77/2023.1

P2X receptors in GtoPdb v.2023.1



Francesco Di Virgilio1, Simonetta Falzoni1, Anna Fortuny-Gomez2, Samuel J. Fountain2, Michael F. Jarvis3, Charles Kennedy4, Brian F. King5, Jessica Meades2, Annette Nicke6 and John A. Peters7
  1. University of Ferrara, Italy
  2. University of East Anglia, UK
  3. University of Illinois, USA
  4. University of Strathclyde, UK
  5. University College London, UK
  6. Ludwig-Maximilians-Universität München, Germany
  7. University of Dundee, UK


Abstract

P2X receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on P2X Receptors [49, 146]) have a trimeric topology [118, 128, 144, 197] with two putative TM domains per P2X subunit, gating primarily Na+, K+ and Ca2+, exceptionally Cl-. The Nomenclature Subcommittee has recommended that for P2X receptors, structural criteria should be the initial basis for nomenclature where possible. X-ray crystallography indicates that functional P2X receptors are trimeric and three agonist molecules are required to bind to a single trimeric assembly in order to activate it [118, 144, 95, 103, 177]. Native receptors may occur as either homotrimers (e.g. P2X1 in smooth muscle) or heterotrimers (e.g. P2X2:P2X3 in the nodose ganglion [280], P2X1:P2X5 in mouse cortical astrocytes [162], and P2X2:P2X5 in mouse dorsal root ganglion, spinal cord and mid pons [53, 234]. P2X2, P2X4 and P2X7 receptor activation can lead to influx of large cationic molecules, such as NMDG+, Yo-Pro, ethidium or propidium iodide [211]. The permeability of the P2X7 receptor is modulated by the amount of cholesterol in the plasma membrane [193]. The hemi-channel pannexin-1 was initially implicated in the action of P2X7 [212], but not P2X2, receptors [41], but this interpretation is probably misleading [215]. Convincing evidence now supports the view that the activated P2X7 receptor is immediately permeable to large cationic molecules, but influx proceeds at a much slower pace than that of the small cations Na+, K+, and Ca2+ [66].

Contents

This is a citation summary for P2X receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [33].

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

P2X receptors
https://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=77
Introduction to P2X receptors
https://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=77
    Channels and Subunits
            P2X1
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=478
            P2X2
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=479
            P2X3
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=480
            P2X4
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=481
            P2X5
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=482
            P2X6
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=483
            P2X7
            https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=484

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