The medicinal chemistry of the P2 receptor family.

Publisher Summary This chapter reviews that the purinoreceptors are a family of receptors that are activated by nucleosides and nucleotides. The purinoreceptors is divided into two families: The P 1 receptors, where nucleosides are more active than nucleotides and the P 2 receptors, where nucleotides are more active than nucleosides. The chapter concentrate on the medicinal chemistry of the P 2 receptor family. It also reviews the P 2 receptor is divided into two major classes, P2X and P2Y. The P2X receptors belong to the ligand-gated cation channel family; whereas the P2Y receptors are members of the seven transmembrane G-protein coupled receptor family. P2X and P2Y receptors are numbered sequentially according to the clone being reported. Capital letters are used to denote functional mammalian receptors or their non-mammalian homologues. Lower case is used to denote orphan mammalian receptors such as receptors having P 2 sequence homology, but no identified functional response and functional non-mammalian receptors with no known mammalian homologue. This system has led to non-sequential numbering of confirmed mammalian P 2 receptors and may necessitate further revision of nomenclature for this class of receptors.