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Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Le Bourdonnec B, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. Le Bourdonnec B, et al. Among authors: graczyk tm. J Med Chem. 2008 Oct 9;51(19):5893-6. doi: 10.1021/jm8008986. Epub 2008 Sep 13. J Med Chem. 2008. PMID: 18788723
Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Le Bourdonnec B, Windh RT, Leister LK, Zhou QJ, Ajello CW, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE. Le Bourdonnec B, et al. Among authors: graczyk tm. J Med Chem. 2009 Sep 24;52(18):5685-702. doi: 10.1021/jm900773n. J Med Chem. 2009. PMID: 19694468
A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine.
DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. DeWire SM, et al. Among authors: graczyk tm. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi: 10.1124/jpet.112.201616. Epub 2013 Jan 8. J Pharmacol Exp Ther. 2013. PMID: 23300227
Novel malonamide derivatives as potent kappa opioid receptor agonists.
Chu GH, Gu M, Cassel JA, Belanger S, Graczyk TM, DeHaven RN, Conway-James N, Koblish M, Little PJ, DeHaven-Hudkins DL, Dolle RE. Chu GH, et al. Among authors: graczyk tm. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1951-5. doi: 10.1016/j.bmcl.2007.01.053. Epub 2007 Jan 25. Bioorg Med Chem Lett. 2007. PMID: 17307360
12 results