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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. 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. J Med Chem. 2009 Sep 24;52(18):5685-702. doi: 10.1021/jm900773n. J Med Chem. 2009. PMID: 19694468
Mu opioid receptor antagonists: recent developments.
Goodman AJ, Le Bourdonnec B, Dolle RE. Goodman AJ, et al. Among authors: le bourdonnec b. ChemMedChem. 2007 Nov;2(11):1552-70. doi: 10.1002/cmdc.200700143. ChemMedChem. 2007. PMID: 17918759 Review.
Novel sulfamoyl benzamides as selective CB(2) agonists with improved in vitro metabolic stability.
Sellitto I, Le Bourdonnec B, Worm K, Goodman A, Savolainen MA, Chu GH, Ajello CW, Saeui CT, Leister LK, Cassel JA, Dehaven RN, Labuda CJ, Koblish M, Little PJ, Brogdon BL, Smith SA, Dolle RE. Sellitto I, et al. Among authors: le bourdonnec b. Bioorg Med Chem Lett. 2010 Jan 1;20(1):387-91. doi: 10.1016/j.bmcl.2009.10.062. Epub 2009 Oct 17. Bioorg Med Chem Lett. 2010. PMID: 19919895
CB2 selective sulfamoyl benzamides: optimization of the amide functionality.
Goodman AJ, Ajello CW, Worm K, Le Bourdonnec B, Savolainen MA, O'Hare H, Cassel JA, Stabley GJ, Dehaven RN, Labuda CJ, Koblish M, Little PJ, Brogdon BL, Smith SA, Dolle RE. Goodman AJ, et al. Among authors: le bourdonnec b. Bioorg Med Chem Lett. 2009 Jan 15;19(2):309-13. doi: 10.1016/j.bmcl.2008.11.091. Epub 2008 Nov 27. Bioorg Med Chem Lett. 2009. PMID: 19091565
The selective mu-opioid receptor antagonist ADL5510 reduces levodopa-induced dyskinesia without affecting antiparkinsonian action in MPTP-lesioned macaque model of Parkinson's disease.
Koprich JB, Fox SH, Johnston TH, Goodman A, Le Bourdonnec B, Dolle RE, DeHaven RN, DeHaven-Hudkins DL, Little PJ, Brotchie JM. Koprich JB, et al. Among authors: le bourdonnec b. Mov Disord. 2011 Jun;26(7):1225-33. doi: 10.1002/mds.23631. Epub 2011 Apr 4. Mov Disord. 2011. PMID: 21465551
33 results