Purinergic Signalling

, Volume 8, Issue 3, pp 375-417

First online:

Open Access This content is freely available online to anyone, anywhere at any time.

Molecular and functional properties of P2X receptors—recent progress and persisting challenges

  • Karina Kaczmarek-HájekAffiliated withMax Planck Institute for Experimental Medicine
  • , Éva LörincziAffiliated withMax Planck Institute for Experimental Medicine
  • , Ralf HausmannAffiliated withMolecular Pharmacology, RWTH Aachen University
  • , Annette NickeAffiliated withMax Planck Institute for Experimental Medicine Email author 


ATP-gated P2X receptors are trimeric ion channels that assemble as homo- or heteromers from seven cloned subunits. Transcripts and/or proteins of P2X subunits have been found in most, if not all, mammalian tissues and are being discovered in an increasing number of non-vertebrates. Both the first crystal structure of a P2X receptor and the generation of knockout (KO) mice for five of the seven cloned subtypes greatly advanced our understanding of their molecular and physiological function and their validation as drug targets. This review summarizes the current understanding of the structure and function of P2X receptors and gives an update on recent developments in the search for P2X subtype-selective ligands. It also provides an overview about the current knowledge of the regulation and modulation of P2X receptors on the cellular level and finally on their physiological roles as inferred from studies on KO mice.


Molecular Functional properties P2X receptors Physiology Pharmacology Protein interactions KO mice