2. Academic Validation
  3. 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

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 Jun 1;28(10):1892-1896. doi: 10.1016/j.bmcl.2018.03.091.
Mark P Healy 1,  Amanda C Allan 2,  Kristin Bailey 2,  Andy Billinton 2,  Iain P Chessell 2,  Nicholas M Clayton 2,  Gerard M P Giblin 2,  Melanie A Kay 2,  Tarik Khaznadar 2,  Anton D Michel 2,  Alan Naylor 2,  Helen Price 2,  David J Spalding 2,  David A Stevens 2,  Martin E Swarbrick 2,  Alexander W Wilson 2
Affiliations

Affiliations

  • 1 GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Electronic address: [email protected].
  • 2 GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
PMID: 29636218 DOI: 10.1016/j.bmcl.2018.03.091
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.

Keywords

Anti-hyperalgesic; Anti-inflammatory; Arthritis; EP4; EP4 receptor agonist; Neuropathic pain; PGE2; Pain; Prostaglandin E2 receptor 4.

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