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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 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. J Med Chem. 1999 Dec 16;42(25):5077-94. doi: 10.1021/jm9806704. J Med Chem. 1999. PMID: 10602693
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
New generation dopaminergic agents. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
Mewshaw RE, Kavanagh J, Stack G, Marquis KL, Shi X, Kagan MZ, Webb MB, Katz AH, Park A, Kang YH, Abou-Gharbia M, Scerni R, Wasik T, Cortes-Burgos L, Spangler T, Brennan JA, Piesla M, Mazandarani H, Cockett MI, Ochalski R, Coupet J, Andree TH. Mewshaw RE, et al. J Med Chem. 1997 Dec 19;40(26):4235-56. doi: 10.1021/jm9703653. J Med Chem. 1997. PMID: 9435894
Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS. Martone RL, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11. J Pharmacol Exp Ther. 2009. PMID: 19671883
78 results