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Page 1
Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y. Elliott RL, et al. Among authors: nardone na. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28. Bioorg Med Chem Lett. 2010. PMID: 20851601
Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
Dow RL, Paight ES, Schneider SR, Hadcock JR, Hargrove DM, Martin KA, Maurer TS, Nardone NA, Tess DA, DaSilva-Jardine P. Dow RL, et al. Among authors: nardone na. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3235-40. doi: 10.1016/j.bmcl.2004.03.089. Bioorg Med Chem Lett. 2004. PMID: 15149682
Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.
Lafontaine JA, Day RF, Dibrino J, Hadcock JR, Hargrove DM, Linhares M, Martin KA, Maurer TS, Nardone NA, Tess DA, Dasilva-Jardine P. Lafontaine JA, et al. Among authors: nardone na. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5245-50. doi: 10.1016/j.bmcl.2007.06.072. Epub 2007 Jun 30. Bioorg Med Chem Lett. 2007. PMID: 17632003
Distribution of beta 3-adrenoceptor mRNA in human tissues.
Berkowitz DE, Nardone NA, Smiley RM, Price DT, Kreutter DK, Fremeau RT, Schwinn DA. Berkowitz DE, et al. Among authors: nardone na. Eur J Pharmacol. 1995 Apr 28;289(2):223-8. doi: 10.1016/0922-4106(95)90098-5. Eur J Pharmacol. 1995. PMID: 7621895
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