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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
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-31 , DOI: 10.1016/j.bmcl.2018.03.091 Mark P. Healy , Amanda C. Allan , Kristin Bailey , Andy Billinton , Iain P. Chessell , Nicholas M. Clayton , Gerard M.P. Giblin , Melanie A. Kay , Tarik Khaznadar , Anton D. Michel , Alan Naylor , Helen Price , David J. Spalding , David A. Stevens , Martin E. Swarbrick , Alexander W. Wilson
中文翻译：
新型{4- [4,9-双（乙氧基）-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基] -2-氟苯基}乙酸（GSK726701A）的发现EP 4受体部分激动剂，用于治疗疼痛
更新日期：2018-03-31
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-03-31 , DOI: 10.1016/j.bmcl.2018.03.091 Mark P. Healy , Amanda C. Allan , Kristin Bailey , Andy Billinton , Iain P. Chessell , Nicholas M. Clayton , Gerard M.P. Giblin , Melanie A. Kay , Tarik Khaznadar , Anton D. Michel , Alan Naylor , Helen Price , David J. Spalding , David A. Stevens , Martin E. Swarbrick , Alexander W. Wilson
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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-clinical models of pain, ultimately leading to the identification of the EP4 partial agonist GSK726701A.
中文翻译：
新型{4- [4,9-双（乙氧基）-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基] -2-氟苯基}乙酸（GSK726701A）的发现EP 4受体部分激动剂，用于治疗疼痛
已经鉴定出一系列新的EP 4激动剂和拮抗剂，然后用于验证其在炎性疼痛治疗中的潜力。本文描述了这些新型配体及其在多种临床前疼痛模型中的活性，最终导致了对EP 4部分激动剂GSK726701A的鉴定。
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