4.5 Article

Discovery of {4-[4,9-bis(ethyloxy)-l-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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 10, Pages 1892-1896

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.091

Keywords

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

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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-chmcal models of pain, ultimately leading to the identification of the EP4 partial agonist GSK726701A. (C) 2018 Elsevier Ltd. All rights reserved.

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