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Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect.
Li Z, Ye R, He Q, Lu J, Sun Y, Sun X, Tang S, Hu S, Chai J, Kong L, Liu X, Chen J, Fang Y, Lan Y, Xie Q, Liu J, Shao L, Fu W, Wang Y, Li W. Li Z, et al. Among authors: wang y. J Med Chem. 2024 May 9;67(9):7112-7129. doi: 10.1021/acs.jmedchem.3c02439. Epub 2024 Apr 22. J Med Chem. 2024. PMID: 38647397
7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.
Sun HJ, Wang YH, Yuan CM, Kong LH, Xu XJ, Wang YJ, Wu HH, Lin C, Qian YY, Huang HM, Xiao L, Liu X, He Q, Fang SY, Xue DQ, Yang XC, Chen H, Zheng YL, Zheng L, Yu LQ, Xie Q, Fu W, Li W, Liu JG, Qiu ZB, Shao LM. Sun HJ, et al. Bioorg Med Chem. 2018 Aug 7;26(14):4254-4263. doi: 10.1016/j.bmc.2018.07.020. Epub 2018 Jul 24. Bioorg Med Chem. 2018. PMID: 30054192
The Pharmacological Heterogeneity of Nepenthone Analogs in Conferring Highly Selective and Potent κ-Opioid Agonistic Activities.
Li W, Long JD, Qian YY, Long Y, Xu XJ, Wang YJ, Shen Q, Wang ZN, Yang XC, Xiao L, Sun HP, Xu YL, Chen YY, Xie Q, Wang YH, Shao LM, Liu JG, Qiu ZB, Fu W. Li W, et al. Among authors: wang yh, wang yj, wang zn. ACS Chem Neurosci. 2017 Apr 19;8(4):766-776. doi: 10.1021/acschemneuro.6b00321. Epub 2017 Jan 19. ACS Chem Neurosci. 2017. PMID: 28033462
Pharmacological characterization and therapeutic potential for the treatment of opioid abuse with ATPM-ET, an N-ethyl substituted aminothiazolomorphinan with κ agonist and μ agonist/antagonist activity.
Sun JF, Wang YH, Chai JR, Li FY, Hang A, Lu G, Tao YM, Cheng Y, Chi ZQ, Neumeyer JL, Zhang A, Liu JG, Wang YJ. Sun JF, et al. Among authors: wang yh, wang yj. Eur J Pharmacol. 2014 Oct 5;740:455-63. doi: 10.1016/j.ejphar.2014.06.045. Epub 2014 Jul 3. Eur J Pharmacol. 2014. PMID: 24998879
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