Discovery of an M -Substituted N -Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile

The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. In this work, a series of -substituted analogs were designed, synthesized, and assayed, resulting in the identification of compound ( ) as a κOR agonist with singl...

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Veröffentlicht in:Journal of medicinal chemistry 2021-08, Vol.64 (16), p.12414-12433
Hauptverfasser: He, Qian, Wei, Yuanyuan, Liu, Xiao, Ye, Rongrong, Kong, Linghui, Li, Zixiang, Jiang, Shuang, Yu, Linqian, Chai, Jingrui, Xie, Qiong, Fu, Wei, Wang, Yujun, Li, Wei, Qiu, Zhuibai, Liu, Jinggen, Shao, Liming
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Sprache:eng
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