P2X receptors C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

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Overview

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P2X receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on P2X Receptors [5,25]) have a trimeric topology [21,24,37] 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 show that functional P2X receptors are trimeric and three agonist molecules are required to bind to a single receptor in order to activate it [12-13,24,30]. Native receptors may occur as either homotrimers (e.g. P2X1 in smooth muscle) or heterotrimers (e.g. P2X2:P2X3 in the nodose ganglion and P2X1:P2X5 in mouse cortical astrocytes, [29]. P2X2, P2X4 and P2X7 receptors have been shown to form functional homopolymers which, in turn, activate pores permeable to low molecular weight solutes [44]. The hemi-channel pannexin-1 has been implicated in the pore formation induced by P2X7 [40], but not P2X2 [4], receptor activation.

Channels and Subunits

P2X1 C Show summary » More detailed page

P2X2 C Show summary » More detailed page

P2X3 C Show summary » More detailed page

P2X4 C Show summary » More detailed page

P2X5 C Show summary » More detailed page

P2X6 C Show summary » More detailed page

P2X7 C Show summary » More detailed page

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Further reading

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Francesco Di Virgilio, Richard J Evans, Simonetta Falzoni, Michael F Jarvis, Charles Kennedy, Brian King, John A. Peters, Baljit S. Khakh, Patrizia Pellegatti. P2X receptors. Accessed on 20/09/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=77.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Peters JA, Kelly E, Marrion N, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Ligand-gated ion channels. Br J Pharmacol. 172: 5870-5903.