Title of article
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
8
From page
3392
To page
3399
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799567
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