化学
兴奋剂
类阿片
药理学
渗透(战争)
慢性疼痛
受体
神经科学
医学
生物化学
心理学
运筹学
工程类
作者
Alok Nerurkar,Thomas Nguyen,S.S.-H. Wang,Ulhas Bhatt,Kevin Li,Yihong Li,Pingyu Ding,Frederick J. Seidl,Martin Holan,John Lee,Tien Widjaja,Zhi‐Liang Wei,Corinne M. Sadlowski,David Sperandio,Lawrence R. McGee,Beth D. Youngblood,Neil Schwartz,Donald R. Gehlert,Julio C. Medina
标识
DOI:10.1016/j.bmcl.2023.129405
摘要
Structural optimization of a previously reported agonist of µOR, PZM21 is described resulting in the discovery of a novel series of amides with at least 4-folds enhanced CNS penetration in rat. Furthermore, these efforts yielded compounds with varying levels of efficacy on the receptor ranging from high efficacy agonists such as compound 20 to antagonists, such as 24. The correlation between in vitro activation of µOR and relative activity in models of analgesia for these compounds is discussed. The compelling results obtained in these studies demonstrate the potential utility of these newly discovered compounds in the treatment of pain and opioid use disorder.
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