Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain.

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Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP4 receptor partial agonist for the treatment of pain.

Bioorg Med Chem Lett. 2018 Mar 31;:

Authors: Healy MP, Allan AC, Bailey K, Billinton A, Chessell IP, Clayton NM, Giblin GMP, Kay MA, Khaznadar T, Michel AD, Naylor A, Price H, Spalding DJ, Stevens DA, Swarbrick ME, Wilson AW

Abstract
A novel series of EP4 agonists and antagonists have been identified, and then used to validate their potential in the treatment of inflammatory pain. This paper describes these novel ligands and their activity within a number of pre-clinical models of pain, ultimately leading to the identification of the EP4 partial agonist GSK726701A.

PMID: 29636218 [PubMed - as supplied by publisher]

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