Author/Authors :
Adrian Hall، نويسنده , , Andy Billinton، نويسنده , , Susan H. Brown، نويسنده , , Nicholas M. Clayton، نويسنده , , Anita Chowdhury، نويسنده , , Gerard M.P. Giblin، نويسنده , , Paul Goldsmith، نويسنده , , Thomas G. Hayhow، نويسنده , , David N. Hurst، نويسنده , , Ian R. Kilford، نويسنده , , Alan Naylor، نويسنده , , Barry Passingham، نويسنده , , Lisa Winyard، نويسنده ,
Abstract :
Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP1 receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.
Keywords :
EP1 antagonist , Non-acidic EP1 antagonist , CNS penetration , pain , In vivo analgesic efficacy
