P2X and P2Y Receptors Kenneth A. Jacobson Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA. Tel.: 301-496- 9024, Fax: 301-480-8422, E-mail:
[email protected] Kenneth Jacobson serves as Chief of the Laboratory of Bioorganic Chemistry and the Molecular Recognition Section at the National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health in Bethesda, Maryland, USA. Dr. Jacobson is a medicinal chemist with interests in the structure and pharmacology of G-protein- coupled receptors, in particular receptors for adenosine and for purine and pyrimidine nucleotides. Contents Subtypes and Structures of P2 Subtypes and Structures of P2 Receptor Families ........ 1 Receptor Families The P2 receptors for extracellular nucleotides are Pharmacological Probes for P2X Receptors .................. 3 widely distributed in the body and participate in 1,2 regulation of nearly every physiological process. DRIVING RESEARCH FURTHER Non-Selective P2X Ligands ............................................ 3 Of particular interest are nucleotide receptors in the immune, inflammatory, cardiovascular, muscular, P2X1 and P2X2 Receptors ............................................... 5 and central and peripheral nervous systems. The ubiquitous signaling properties of extracellular P2X3 Receptor ................................................................ 6 nucleotides acting at two