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A promising chemical series of positive allosteric modulators of the μ-opioid receptor that enhance the antinociceptive efficacy of opioids but not their adverse effects.
Pryce KD, Kang HJ, Sakloth F, Liu Y, Khan S, Toth K, Kapoor A, Nicolais A, Che T, Qin L, Bertherat F, Kaniskan HÜ, Jin J, Cameron MD, Roth BL, Zachariou V, Filizola M. Pryce KD, et al. Neuropharmacology. 2021 Sep 1;195:108673. doi: 10.1016/j.neuropharm.2021.108673. Epub 2021 Jun 18. Neuropharmacology. 2021. PMID: 34153316 Free PMC article.
A Novel Mitragynine Analog with Low-Efficacy Mu Opioid Receptor Agonism Displays Antinociception with Attenuated Adverse Effects.
Chakraborty S, DiBerto JF, Faouzi A, Bernhard SM, Gutridge AM, Ramsey S, Zhou Y, Provasi D, Nuthikattu N, Jilakara R, Nelson MNF, Asher WB, Eans SO, Wilson LL, Chintala SM, Filizola M, van Rijn RM, Margolis EB, Roth BL, McLaughlin JP, Che T, Sames D, Javitch JA, Majumdar S. Chakraborty S, et al. J Med Chem. 2021 Sep 23;64(18):13873-13892. doi: 10.1021/acs.jmedchem.1c01273. Epub 2021 Sep 10. J Med Chem. 2021. PMID: 34505767 Free PMC article.