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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: childers we. 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. 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.
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
Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents.
Abou-Gharbia MA, Childers WE Jr, Fletcher H, McGaughey G, Patel U, Webb MB, Yardley J, Andree T, Boast C, Kucharik RJ Jr, Marquis K, Morris H, Scerni R, Moyer JA. Abou-Gharbia MA, et al. Among authors: childers we jr. J Med Chem. 1999 Dec 16;42(25):5077-94. doi: 10.1021/jm9806704. J Med Chem. 1999. PMID: 10602693
Prodrugs of perzinfotel with improved oral bioavailability.
Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE Jr. Baudy RB, et al. Among authors: childers we jr. J Med Chem. 2009 Feb 12;52(3):771-8. doi: 10.1021/jm8011799. J Med Chem. 2009. PMID: 19146418
3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.
Havran LM, Chong DC, Childers WE, Dollings PJ, Dietrich A, Harrison BL, Marathias V, Tawa G, Aulabaugh A, Cowling R, Kapoor B, Xu W, Mosyak L, Moy F, Hum WT, Wood A, Robichaud AJ. Havran LM, et al. Among authors: childers we. Bioorg Med Chem. 2009 Nov 15;17(22):7755-68. doi: 10.1016/j.bmc.2009.09.036. Epub 2009 Sep 24. Bioorg Med Chem. 2009. PMID: 19836248
56 results