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Page 1
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Dosa PI, Covel JA, Ren A, Webb RR, Beeley NR, Martin M, Morgan M, Espitia S, Saldana HR, Bjenning C, Whelan KT, Grottick AJ, Menzaghi F, Thomsen WJ. Smith BM, et al. Among authors: ren a. J Med Chem. 2008 Jan 24;51(2):305-13. doi: 10.1021/jm0709034. Epub 2007 Dec 21. J Med Chem. 2008. PMID: 18095642
A new family of H3 receptor antagonists based on the natural product Conessine.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ. Santora VJ, et al. Among authors: ren a. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059. Epub 2007 Dec 25. Bioorg Med Chem Lett. 2008. PMID: 18194865
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ. Santora VJ, et al. Among authors: ren a. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4133-6. doi: 10.1016/j.bmcl.2008.05.086. Epub 2008 May 24. Bioorg Med Chem Lett. 2008. PMID: 18554904
Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Semple G, Ren A, Fioravanti B, Pereira G, Calderon I, Choi K, Xiong Y, Shin YJ, Gharbaoui T, Sage CR, Morgan M, Xing C, Chu ZL, Leonard JN, Grottick AJ, Al-Shamma H, Liang Y, Demarest KT, Jones RM. Semple G, et al. Among authors: ren a. Bioorg Med Chem Lett. 2011 May 15;21(10):3134-41. doi: 10.1016/j.bmcl.2011.03.007. Epub 2011 Mar 13. Bioorg Med Chem Lett. 2011. PMID: 21444206
Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Semple G, Lehmann J, Wong A, Ren A, Bruce M, Shin YJ, Sage CR, Morgan M, Chen WC, Sebring K, Chu ZL, Leonard JN, Al-Shamma H, Grottick AJ, Du F, Liang Y, Demarest K, Jones RM. Semple G, et al. Among authors: ren a. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1750-5. doi: 10.1016/j.bmcl.2011.12.092. Epub 2011 Dec 30. Bioorg Med Chem Lett. 2012. PMID: 22264481
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT2C receptor.
Schrader TO, Zhu X, Kasem M, Ren A, Liu C, Wu C, Dang H, Le M, Gatlin J, Chase K, Frazer J, Whelan KT, Grottick AJ, Hutton C, Barden J, Chen C, Ortiz A, Feichtinger K, Semple G. Schrader TO, et al. Among authors: ren a. Bioorg Med Chem Lett. 2021 Apr 15;38:127872. doi: 10.1016/j.bmcl.2021.127872. Epub 2021 Feb 23. Bioorg Med Chem Lett. 2021. PMID: 33636307
Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.
Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. Semple G, et al. Among authors: ren a. J Med Chem. 2008 Sep 11;51(17):5172-5. doi: 10.1021/jm8006867. Epub 2008 Aug 13. J Med Chem. 2008. PMID: 18698756
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.
Covel JA, Santora VJ, Smith JM, Hayashi R, Gallardo C, Weinhouse MI, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Pulley MD, Smith BM, Ren A, Suarez M, Frazer J, Edwards J, Hauser EK, Lorea J, Semple G, Grottick AJ. Covel JA, et al. Among authors: ren a. J Med Chem. 2009 Sep 24;52(18):5603-11. doi: 10.1021/jm900857n. J Med Chem. 2009. PMID: 19722526
1,012 results