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Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405).
Hirst WD, Andree TH, Aschmies S, Childers WE, Comery TA, Dawson LA, Day M, Feingold IB, Grauer SM, Harrison BL, Hughes ZA, Kao J, Kelly MG, van der Lee H, Rosenzweig-Lipson S, Saab AL, Smith DL, Sullivan K, Rizzo SJ, Tio C, Zhang MY, Schechter LE. Hirst WD, et al. Among authors: sullivan k. J Pharmacol Exp Ther. 2008 Apr;325(1):134-45. doi: 10.1124/jpet.107.133082. Epub 2008 Jan 8. J Pharmacol Exp Ther. 2008. PMID: 18182558
Preclinical characterization of WAY-211612: a dual 5-HT uptake inhibitor and 5-HT (1A) receptor antagonist and potential novel antidepressant.
Beyer CE, Lin Q, Platt B, Malberg J, Hornby G, Sullivan KM, Smith DL, Lock T, Mitchell PJ, Hatzenbuhler NT, Evrard DA, Harrison BL, Magolda R, Pangalos MN, Schechter LE, Rosenzweig-Lipson S, Andree TH. Beyer CE, et al. Among authors: sullivan km. Br J Pharmacol. 2009 May;157(2):307-19. doi: 10.1111/j.1476-5381.2009.00146.x. Epub 2009 Mar 26. Br J Pharmacol. 2009. PMID: 19338583 Free PMC article.
Aplindore (DAB-452), a high affinity selective dopamine D2 receptor partial agonist.
Heinrich JN, Brennan J, Lai MH, Sullivan K, Hornby G, Popiolek M, Jiang LX, Pausch MH, Stack G, Marquis KL, Andree TH. Heinrich JN, et al. Among authors: sullivan k. Eur J Pharmacol. 2006 Dec 15;552(1-3):36-45. doi: 10.1016/j.ejphar.2006.08.063. Epub 2006 Sep 14. Eur J Pharmacol. 2006. PMID: 17056032
Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Hatzenbuhler NT, Evrard DA, Harrison BL, Huryn D, Inghrim J, Kraml C, Mattes JF, Mewshaw RE, Zhou D, Hornby G, Lin Q, Smith DL, Sullivan KM, Schechter LE, Beyer CE, Andree TH. Hatzenbuhler NT, et al. J Med Chem. 2006 Jul 27;49(15):4785-9. doi: 10.1021/jm060218h. J Med Chem. 2006. PMID: 16854086
Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT(1A) receptor and the serotonin transporter.
Shen Z, Siva Ramamoorthy P, Hatzenbuhler NT, Evrard DA, Childers W, Harrison BL, Chlenov M, Hornby G, Smith DL, Sullivan KM, Schechter LE, Andree TH. Shen Z, et al. Bioorg Med Chem Lett. 2010 Jan 1;20(1):222-7. doi: 10.1016/j.bmcl.2009.10.134. Epub 2009 Oct 31. Bioorg Med Chem Lett. 2010. PMID: 19932965
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
Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2.
Hatzenbuhler NT, Baudy R, Evrard DA, Failli A, Harrison BL, Lenicek S, Mewshaw RE, Saab A, Shah U, Sze J, Zhang M, Zhou D, Chlenov M, Kagan M, Golembieski J, Hornby G, Lai M, Smith DL, Sullivan KM, Schechter LE, Andree TH. Hatzenbuhler NT, et al. J Med Chem. 2008 Nov 13;51(21):6980-7004. doi: 10.1021/jm8007097. Epub 2008 Oct 4. J Med Chem. 2008. PMID: 18834188
2,953 results