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P2X receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Di Virgilio, F; Evans, RJ; Falzoni, S; Jarvis, MF; Kennedy, C; Khakh, BS; King, BF; ... Peters, JA; + view all (2019) P2X receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE , 2019 (4) 10.2218/gtopdb/F77/2019.4. Green open access

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Abstract

P2X receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on P2X Receptors [46, 134]) have a trimeric topology [118, 132, 177] with two putative TM domains, gating primarily Na+, K+ and Ca2+, exceptionally Cl-. The Nomenclature Subcommittee has recommended that for P2X receptors, structural criteria should be the initial criteria 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 receptor in order to activate it [132, 88, 96, 161]. Native receptors may occur as either homotrimers (e.g. P2X1 in smooth muscle) or heterotrimers (e.g. P2X2:P2X3 in the nodose ganglion [251], P2X1:P2X5 in mouse cortical astrocytes [146], and P2X2:P2X5 in mouse dorsal root ganglion, spinal cord and mid pons [50, 207]. P2X2, P2X4 and P2X7 receptors have been shown to form functional homopolymers which, in turn, activate pores permeable to low molecular weight solutes [229]. The hemi-channel pannexin-1 has been implicated in the pore formation induced by P2X7 [188], but not P2X2 [38], receptor activation.

Type: Article
Title: P2X receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Open access status: An open access version is available from UCL Discovery
DOI: 10.2218/gtopdb/F77/2019.4
Publisher version: https://doi.org/10.2218/gtopdb/F77/2019.4
Language: English
Additional information: This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License (http://creativecommons.org/licenses/by-sa/4.0/).
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: https://discovery.ucl.ac.uk/id/eprint/10106879
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