Ontology highlight
ABSTRACT:
SUBMITTER: Jarvis MF
PROVIDER: S-EPMC139289 | biostudies-literature | 2002 Dec
REPOSITORIES: biostudies-literature
Jarvis Michael F MF Burgard Edward C EC McGaraughty Steve S Honore Prisca P Lynch Kevin K Brennan Timothy J TJ Subieta Alberto A Van Biesen Tim T Cartmell Jayne J Bianchi Bruce B Niforatos Wende W Kage Karen K Yu Haixia H Mikusa Joe J Wismer Carol T CT Zhu Chang Z CZ Chu Katharine K Lee Chih-Hung CH Stewart Andrew O AO Polakowski James J Cox Bryan F BF Kowaluk Elizabeth E Williams Michael M Sullivan James J Faltynek Connie C
Proceedings of the National Academy of Sciences of the United States of America 20021213 26
P2X3 and P2X2/3 receptors are highly localized on peripheral and central processes of sensory afferent nerves, and activation of these channels contributes to the pronociceptive effects of ATP. A-317491 is a novel non-nucleotide antagonist of P2X3 and P2X2/3 receptor activation. A-317491 potently blocked recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and was highly selective (IC50 >10 microM) over other P2 receptors and other neurotransmitter receptors, ...[more]