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Page 1
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: semple g. 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
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: semple g. 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: semple g. 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
Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG. Boatman PD, et al. Among authors: semple g. Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20. Bioorg Med Chem Lett. 2010. PMID: 20363624
Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomnia.
Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Dosa PI, Feichtinger K, Teegarden BR, Frazer JM, Yoon WH, Shan Y, Whelan K, Hauser EK, Grottick AJ, Semple G, Al-Shamma H. Xiong Y, et al. Among authors: semple g. J Med Chem. 2010 Aug 12;53(15):5696-706. doi: 10.1021/jm100479q. J Med Chem. 2010. PMID: 20684606
Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.
Xiong Y, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Feichtinger K, Frazer JM, Yoon WH, Whelan K, Sanabria EK, Grottick AJ, Al-Shamma H, Semple G. Xiong Y, et al. Among authors: semple g. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1870-3. doi: 10.1016/j.bmcl.2012.01.080. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325948
Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.
Han S, Thoresen L, Zhu X, Narayanan S, Jung JK, Strah-Pleynet S, Decaire M, Choi K, Xiong Y, Yue D, Semple G, Thatte J, Solomon M, Fu L, Whelan K, Al-Shamma H, Gatlin J, Chen R, Dang H, Pride C, Gaidarov I, Unett DJ, Behan DP, Sadeque A, Usmani KA, Chen C, Edwards J, Morgan M, Jones RM. Han S, et al. Among authors: semple g. Bioorg Med Chem Lett. 2015 Jan 15;25(2):322-6. doi: 10.1016/j.bmcl.2014.11.040. Epub 2014 Nov 26. Bioorg Med Chem Lett. 2015. PMID: 25488844
Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays.
Ren A, Zhu X, Feichtinger K, Lehman J, Kasem M, Schrader TO, Wong A, Dang H, Le M, Frazer J, Unett DJ, Grottick AJ, Whelan KT, Morgan ME, Sage CR, Semple G. Ren A, et al. Among authors: semple g. Bioorg Med Chem Lett. 2020 Mar 1;30(5):126929. doi: 10.1016/j.bmcl.2019.126929. Epub 2019 Dec 26. Bioorg Med Chem Lett. 2020. PMID: 31952960
Agonist lead identification for the high affinity niacin receptor GPR109a.
Gharbaoui T, Skinner PJ, Shin YJ, Averbuj C, Jung JK, Johnson BR, Duong T, Decaire M, Uy J, Cherrier MC, Webb PJ, Tamura SY, Zou N, Rodriguez N, Boatman PD, Sage CR, Lindstrom A, Xu J, Schrader TO, Smith BM, Chen R, Richman JG, Connolly DT, Colletti SL, Tata JR, Semple G. Gharbaoui T, et al. Among authors: semple g. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4914-9. doi: 10.1016/j.bmcl.2007.06.028. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17588745
80 results