Therapeutic applications of ATP-(P2)-receptors agonists and antagonists

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P2-receptors (P2-R), which recognise extracellular ATP, represent significant targets for novel drug development regarding different pathophysiological conditions. In recent years, approximately fifteen ATP receptor subtypes have been cloned; seven of which belong to the P2X-R family (ligand-gated-ion-channel receptors). The remaining subtypes belong to the P2Y-R family (G-protein coupled receptors). These receptors have been classified based on their putative molecular structure, function, and the action of a subtype selective drug on the cloned receptor. A limited number of reports describe the identification of potent and selective P2X/P2Y agonists, thus extending the restricted arsenal of P2-R agonists consisting primarily of commercial compounds. Several new and subtype selective antagonists have been recently identified which open a new avenue of P2X or P2Y subtype selective antagonists for receptor studies. Current applications of P2-R agonists and antagonists include their use as insulin secretagogues, inhibitors of ADP-induced platelet aggregation, agents for hydration of lung mucous in cystic fibrosis (CF) patients, modulators of cardiac muscle contractility, and antineoplastic agents. This paper reviews selected P2-R related publications and patents issued between 1995 and 1998 for newly cloned P2-R, drug candidates, and the potential therapeutic applications of the drugs.

Original languageEnglish
Pages (from-to)385-399
Number of pages15
JournalExpert Opinion on Therapeutic Patents
Issue number4
StatePublished - 1999


  • ATP
  • ATP-analogue
  • Agonist
  • Antagonist
  • Antineoplastic agents
  • Cardiovascular system
  • Cystic fibrosis
  • Insulin secretion
  • Ischaemia-reperfusion injury
  • P2X-receptor
  • P2Y-receptor
  • Platelet aggregation


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