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Page 1
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. Among authors: huselton c. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Zhou D, Stack GP, Lo J, Failli AA, Evrard DA, Harrison BL, Hatzenbuhler NT, Tran M, Croce S, Yi S, Golembieski J, Hornby GA, Lai M, Lin Q, Schechter LE, Smith DL, Shilling AD, Huselton C, Mitchell P, Beyer CE, Andree TH. Zhou D, et al. Among authors: huselton c. J Med Chem. 2009 Aug 13;52(15):4955-9. doi: 10.1021/jm900374r. J Med Chem. 2009. PMID: 19719241
5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.
Haydar SN, Yun H, Andrae PM, Mattes J, Zhang J, Kramer A, Smith DL, Huselton C, Graf R, Aschmies S, Schechter LE, Comery TA, Robichaud AJ. Haydar SN, et al. Among authors: huselton c. J Med Chem. 2010 Mar 25;53(6):2521-7. doi: 10.1021/jm901674f. J Med Chem. 2010. PMID: 20170099
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
Heffernan GD, Coghlan RD, Manas ES, McDevitt RE, Li Y, Mahaney PE, Robichaud AJ, Huselton C, Alfinito P, Bray JA, Cosmi SA, Johnston GH, Kenney T, Koury E, Winneker RC, Deecher DC, Trybulski EJ. Heffernan GD, et al. Among authors: huselton c. Bioorg Med Chem. 2009 Nov 15;17(22):7802-15. doi: 10.1016/j.bmc.2009.09.023. Epub 2009 Sep 18. Bioorg Med Chem. 2009. PMID: 19836247
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Blass BE, Fensome A, Trybulski E, Magolda R, Gardell SJ, Liu K, Samuel M, Feingold I, Huselton C, Jackson CM, Djandjighian L, Ho D, Hennan J, Janusz JM. Blass BE, et al. Among authors: huselton c. J Med Chem. 2009 Nov 12;52(21):6531-4. doi: 10.1021/jm901042m. J Med Chem. 2009. PMID: 19888755
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Pelletier JC, Chengalvala MV, Cottom JE, Feingold IB, Green DM, Hauze DB, Huselton CA, Jetter JW, Kopf GS, Lundquist JT, Magolda RL, Mann CW, Mehlmann JF, Rogers JF, Shanno LK, Adams WR, Tio CO, Wrobel JE. Pelletier JC, et al. Among authors: huselton ca. J Med Chem. 2009 Apr 9;52(7):2148-52. doi: 10.1021/jm801572m. J Med Chem. 2009. PMID: 19271735
The metabotropic glutamate receptor 7 allosteric modulator AMN082: a monoaminergic agent in disguise?
Sukoff Rizzo SJ, Leonard SK, Gilbert A, Dollings P, Smith DL, Zhang MY, Di L, Platt BJ, Neal S, Dwyer JM, Bender CN, Zhang J, Lock T, Kowal D, Kramer A, Randall A, Huselton C, Vishwanathan K, Tse SY, Butera J, Ring RH, Rosenzweig-Lipson S, Hughes ZA, Dunlop J. Sukoff Rizzo SJ, et al. Among authors: huselton c. J Pharmacol Exp Ther. 2011 Jul;338(1):345-52. doi: 10.1124/jpet.110.177378. Epub 2011 Apr 20. J Pharmacol Exp Ther. 2011. PMID: 21508084
Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ. Wrobel J, et al. Among authors: huselton c. J Med Chem. 2008 Nov 27;51(22):7161-8. doi: 10.1021/jm800799q. J Med Chem. 2008. PMID: 18973288
38 results