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Page 1
Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.
Rotella DP, McFarlane GR, Greenfield A, Grosanu C, Robichaud AJ, Denny RA, Feenstra RW, Núñez-García S, Reinders JH, Neut Mv, McCreary A, Kruse CG, Sullivan K, Pruthi F, Lai M, Zhang J, Kowal DM, Carrick T, Grauer SM, Navarra RL, Graf R, Brennan J, Marquis KL, Pausch MH. Rotella DP, et al. Among authors: grauer sm. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5552-5. doi: 10.1016/j.bmcl.2009.08.050. Epub 2009 Aug 15. Bioorg Med Chem Lett. 2009. PMID: 19720528
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. Among authors: grauer sm. 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
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ. Malamas MS, et al. J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11. J Med Chem. 2011. PMID: 21988093
Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N. Malamas MS, et al. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31. Bioorg Med Chem Lett. 2012. PMID: 22902656
Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia.
Grauer SM, Pulito VL, Navarra RL, Kelly MP, Kelley C, Graf R, Langen B, Logue S, Brennan J, Jiang L, Charych E, Egerland U, Liu F, Marquis KL, Malamas M, Hage T, Comery TA, Brandon NJ. Grauer SM, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90. doi: 10.1124/jpet.109.155994. Epub 2009 Aug 6. J Pharmacol Exp Ther. 2009. PMID: 19661377
The orphan GPCR, GPR88, modulates function of the striatal dopamine system: a possible therapeutic target for psychiatric disorders?
Logue SF, Grauer SM, Paulsen J, Graf R, Taylor N, Sung MA, Zhang L, Hughes Z, Pulito VL, Liu F, Rosenzweig-Lipson S, Brandon NJ, Marquis KL, Bates B, Pausch M. Logue SF, et al. Among authors: grauer sm. Mol Cell Neurosci. 2009 Dec;42(4):438-47. doi: 10.1016/j.mcn.2009.09.007. Epub 2009 Sep 29. Mol Cell Neurosci. 2009. PMID: 19796684
ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities.
Liu F, Grauer S, Kelley C, Navarra R, Graf R, Zhang G, Atkinson PJ, Popiolek M, Wantuch C, Khawaja X, Smith D, Olsen M, Kouranova E, Lai M, Pruthi F, Pulicicchio C, Day M, Gilbert A, Pausch MH, Brandon NJ, Beyer CE, Comery TA, Logue S, Rosenzweig-Lipson S, Marquis KL. Liu F, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. doi: 10.1124/jpet.108.136580. Epub 2008 Aug 27. J Pharmacol Exp Ther. 2008. PMID: 18753411
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Ghiron C, Haydar SN, Aschmies S, Bothmann H, Castaldo C, Cocconcelli G, Comery TA, Di L, Dunlop J, Lock T, Kramer A, Kowal D, Jow F, Grauer S, Harrison B, La Rosa S, Maccari L, Marquis KL, Micco I, Nencini A, Quinn J, Robichaud AJ, Roncarati R, Scali C, Terstappen GC, Turlizzi E, Valacchi M, Varrone M, Zanaletti R, Zanelli U. Ghiron C, et al. J Med Chem. 2010 Jun 10;53(11):4379-89. doi: 10.1021/jm901692q. J Med Chem. 2010. PMID: 20465311
26 results