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Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE. Cole DC, et al. J Med Chem. 2007 Nov 15;50(23):5535-8. doi: 10.1021/jm070521y. Epub 2007 Oct 19. J Med Chem. 2007. PMID: 17948978
WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: a novel dopamine D2 receptor partial agonist/serotonin reuptake inhibitor with preclinical antipsychotic-like and antidepressant-like activity.
Brennan JA, Graf R, Grauer SM, Navarra RL, Pulicicchio CM, Hughes ZA, Lin Q, Wantuch C, Rosenzweig-Lipson S, Pruthi F, Lai M, Smith D, Goutier W, van de Neut M, Robichaud AJ, Rotella D, Feenstra RW, Kruse C, Broqua P, Beyer CE, McCreary AC, Pausch MH, Marquis KL. Brennan JA, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):190-201. doi: 10.1124/jpet.109.157388. Epub 2009 Oct 14. J Pharmacol Exp Ther. 2010. PMID: 19828876
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD. Childers WE Jr, et al. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
76 results