发现 4-[4,9-双（乙氧基）-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基]-2-氟苯乙酸（GSK726701A），一种新型的 EP 受体部分激动剂，用于治疗疼痛。
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 EP receptor partial agonist for the treatment of pain.
机构信息
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
出版信息
Bioorg Med Chem Lett. 2018 Jun 1;28(10):1892-1896. doi: 10.1016/j.bmcl.2018.03.091. Epub 2018 Mar 31.
A novel series of EP 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 EP partial agonist GSK726701A.
已经鉴定出一系列新型 EP 激动剂和拮抗剂，然后用于验证它们在治疗炎症性疼痛方面的潜力。本文描述了这些新型配体及其在多种疼痛临床前模型中的活性，最终导致 EP 部分激动剂 GSK726701A 的鉴定。
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