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  • Title: Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
    Author: Hall A, Billinton A, Brown SH, Clayton NM, Chowdhury A, Giblin GM, Goldsmith P, Hayhow TG, Hurst DN, Kilford IR, Naylor A, Passingham B, Winyard L.
    Journal: Bioorg Med Chem Lett; 2008 Jun 01; 18(11):3392-9. PubMed ID: 18462938.
    Abstract:
    Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) 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.
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