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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: smith dl. 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
Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties.
Schechter LE, Smith DL, Rosenzweig-Lipson S, Sukoff SJ, Dawson LA, Marquis K, Jones D, Piesla M, Andree T, Nawoschik S, Harder JA, Womack MD, Buccafusco J, Terry AV, Hoebel B, Rada P, Kelly M, Abou-Gharbia M, Barrett JE, Childers W. Schechter LE, et al. Among authors: smith dl. J Pharmacol Exp Ther. 2005 Sep;314(3):1274-89. doi: 10.1124/jpet.105.086363. Epub 2005 Jun 10. J Pharmacol Exp Ther. 2005. PMID: 15951399 Free article.
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: smith dl. 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.
Studies towards the next generation of antidepressants. Part 4: derivatives of 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.
Evrard DA, Zhou P, Yi SY, Zhou D, Smith DL, Sullivan KM, Hornby GA, Schechter LE, Andree TH, Mewshaw RE. Evrard DA, et al. Among authors: smith dl. Bioorg Med Chem Lett. 2005 Feb 15;15(4):911-4. doi: 10.1016/j.bmcl.2004.12.064. Bioorg Med Chem Lett. 2005. PMID: 15686885
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
Childers WE Jr, Abou-Gharbia MA, Kelly MG, Andree TH, Harrison BL, Ho DM, Hornby G, Huryn DM, Potestio L, Rosenzweig-Lipson SJ, Schmid J, Smith DL, Sukoff SJ, Zhang G, Schechter LE. Childers WE Jr, et al. Among authors: smith dl. J Med Chem. 2005 May 19;48(10):3467-70. doi: 10.1021/jm049493z. J Med Chem. 2005. PMID: 15887953
Studies toward the discovery of the next generation of antidepressants. Part 5: 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Zhou D, Harrison BL, Shah U, Andree TH, Hornby GA, Scerni R, Schechter LE, Smith DL, Sullivan KM, Mewshaw RE. Zhou D, et al. Among authors: smith dl. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1338-41. doi: 10.1016/j.bmcl.2005.11.054. Epub 2005 Dec 5. Bioorg Med Chem Lett. 2006. PMID: 16332439
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. Among authors: smith dl. J Med Chem. 2006 Jul 27;49(15):4785-9. doi: 10.1021/jm060218h. J Med Chem. 2006. PMID: 16854086
1,623 results