Discovery, structure-activity relationship studies, and anti-nociceptive effects of N-(1,2,3,4-tetrahydro-1-isoquinolinylmethyl)benzamides as novel opioid receptor agonists

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• 作者：Sheng-Ren Chen^a ; ^c ; Yi-Yu Ke^a ; ¹ ; Teng-Kuang Yeh^a ; ¹ ; Shu-Yu Lin^a ; Li-Chin Ou^a ; Shu-Chun Chen^a ; Wan-Ting Chang^a ; Hsiao-Fu Chang^a ; Zih-Huei Wu^a ; Chih-Chien Hsieh^a ; Ping-Yee Law^b ; Horace H. Loh^b ; Chuan Shih^a ; Yiu-Kay Lai^c ; ^{yklai@life.nthu.edu.tw} ; Shiu-Hwa Yeh^a ; ^d ; ^{bau9763@bp.nhri.org.tw} ; Shau-Hua Ueng^a ; ^{shueng@nhri.org.tw}
• 关键词：μ-opioid receptor agonist ; κ-opioid receptor agonist ; Structure-activity relationship ; Blood-brain barrier ; Penetration ; Anti-nociceptive effects ; Tail-flick test
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：202-217
• 全文大小：1858 K
• 卷排序：126

文摘

Structural modification resulted in a series of μ/κ-opioid receptor agonists. Compound 46 demonstrated potent anti-nociceptive effect in B6 mice. A molecular docking of 46 predicted the potential binding site in μ-opioid receptor.