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134 related items for PubMed ID: 20443629

  • 1. The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
    Childers WE, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC, 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.
    J Med Chem; 2010 May 27; 53(10):4066-84. PubMed ID: 20443629
    [Abstract] [Full Text] [Related]

  • 2. 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.
    J Pharmacol Exp Ther; 2008 Apr 27; 325(1):134-45. PubMed ID: 18182558
    [Abstract] [Full Text] [Related]

  • 3. Synthesis and SAR of highly potent dual 5-HT1A and 5-HT1B antagonists as potential antidepressant drugs.
    Kling A, Lange UE, Mack H, Bakker MH, Drescher KU, Hornberger W, Hutchins CW, Möller A, Müller R, Schmidt M, Unger L, Wicke K, Schellhaas K, Steiner G.
    Bioorg Med Chem Lett; 2005 Dec 15; 15(24):5567-73. PubMed ID: 16219465
    [Abstract] [Full Text] [Related]

  • 4. Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
    Childers WE, 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.
    J Med Chem; 2005 May 19; 48(10):3467-70. PubMed ID: 15887953
    [Abstract] [Full Text] [Related]

  • 5. 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.
    J Pharmacol Exp Ther; 2005 Sep 19; 314(3):1274-89. PubMed ID: 15951399
    [Abstract] [Full Text] [Related]

  • 6. S 15535, a novel benzodioxopiperazine ligand of serotonin (5-HT)1A receptors: I. Interaction with cloned human (h)5-HT1A, dopamine hD2/hD3 and h alpha2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in models of potential antidepressant activity.
    Millan MJ, Newman-Tancredi A, Rivet JM, Brocco M, Lacroix P, Audinot V, Cistarelli L, Gobert A.
    J Pharmacol Exp Ther; 1997 Jul 19; 282(1):132-47. PubMed ID: 9223549
    [Abstract] [Full Text] [Related]

  • 7. Optimization of (arylpiperazinylbutyl)oxindoles exhibiting selective 5-HT₇ receptor antagonist activity.
    Volk B, Gacsályi I, Pallagi K, Poszávácz L, Gyönös I, Szabó E, Bakó T, Spedding M, Simig G, Szénási G.
    J Med Chem; 2011 Oct 13; 54(19):6657-69. PubMed ID: 21859099
    [Abstract] [Full Text] [Related]

  • 8. New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
    Jurczyk S, Kołaczkowski M, Maryniak E, Zajdel P, Pawłowski M, Tatarczyńska E, Kłodzińska A, Chojnacka-Wójcik E, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Nowak G, Maciag D.
    J Med Chem; 2004 May 06; 47(10):2659-66. PubMed ID: 15115407
    [Abstract] [Full Text] [Related]

  • 9. N-[omega-[4-(2-methoxyphenyl)-1-piperazinyl]alkyl]-2-quinolinamines as high-affinity fluorescent 5-HT1A receptor ligands.
    Lacivita E, Leopoldo M.
    J Med Chem; 2008 Mar 13; 51(5):1492-5. PubMed ID: 18269229
    [Abstract] [Full Text] [Related]

  • 10. Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
    Ward SE, Eddershaw PJ, Scott CM, Gordon LJ, Lovell PJ, Moore SH, Smith PW, Starr KR, Thewlis KM, Watson JM.
    J Med Chem; 2008 May 22; 51(10):2887-90. PubMed ID: 18433113
    [Abstract] [Full Text] [Related]

  • 11. Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
    Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C, Kleven M.
    J Med Chem; 1999 May 06; 42(9):1648-60. PubMed ID: 10229633
    [Abstract] [Full Text] [Related]

  • 12. The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis.
    Millan MJ, Gobert A, Roux S, Porsolt R, Meneses A, Carli M, Di Cara B, Jaffard R, Rivet JM, Lestage P, Mocaer E, Peglion JL, Dekeyne A.
    J Pharmacol Exp Ther; 2004 Oct 06; 311(1):190-203. PubMed ID: 15146031
    [Abstract] [Full Text] [Related]

  • 13. Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
    Peglion JL, Goument B, Despaux N, Charlot V, Giraud H, Nisole C, Newman-Tancredi A, Dekeyne A, Bertrand M, Genissel P, Millan MJ.
    J Med Chem; 2002 Jan 03; 45(1):165-76. PubMed ID: 11754589
    [Abstract] [Full Text] [Related]

  • 14. 5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.
    Liu KG, Robichaud AJ, Bernotas RC, Yan Y, Lo JR, Zhang MY, Hughes ZA, Huselton C, Zhang GM, Zhang JY, Kowal DM, Smith DL, Schechter LE, Comery TA.
    J Med Chem; 2010 Nov 11; 53(21):7639-46. PubMed ID: 20932009
    [Abstract] [Full Text] [Related]

  • 15. In vitro profile of the antidepressant candidate OPC-14523 at rat and human 5-HT1A receptors.
    Jordan S, Chen R, Koprivica V, Hamilton R, Whitehead RE, Tottori K, Kikuchi T.
    Eur J Pharmacol; 2005 Jul 11; 517(3):165-73. PubMed ID: 15985260
    [Abstract] [Full Text] [Related]

  • 16. Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
    Mewshaw RE, Zhou D, Zhou P, Shi X, Hornby G, Spangler T, Scerni R, Smith D, Schechter LE, Andree TH.
    J Med Chem; 2004 Jul 15; 47(15):3823-42. PubMed ID: 15239661
    [Abstract] [Full Text] [Related]

  • 17. A longitudinal study of 5-HT outflow during chronic fluoxetine treatment using a new technique of chronic microdialysis in a highly emotional mouse strain.
    Popa D, Cerdan J, Repérant C, Guiard BP, Guilloux JP, David DJ, Gardier AM.
    Eur J Pharmacol; 2010 Feb 25; 628(1-3):83-90. PubMed ID: 19944680
    [Abstract] [Full Text] [Related]

  • 18. (R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.
    Tatsumi R, Fujio M, Takanashi S, Numata A, Katayama J, Satoh H, Shiigi Y, Maeda J, Kuriyama M, Horikawa T, Murozono T, Hashimoto K, Tanaka H.
    J Med Chem; 2006 Jul 13; 49(14):4374-83. PubMed ID: 16821797
    [Abstract] [Full Text] [Related]

  • 19. Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor-5-HT1A/5-HT2A/5-HT7 and D2/D3/D4-agents: the synthesis and pharmacological evaluation.
    Zajdel P, Marciniec K, Maślankiewicz A, Satała G, Duszyńska B, Bojarski AJ, Partyka A, Jastrzębska-Więsek M, Wróbel D, Wesołowska A, Pawłowski M.
    Bioorg Med Chem; 2012 Feb 15; 20(4):1545-56. PubMed ID: 22277589
    [Abstract] [Full Text] [Related]

  • 20. Serotonin 5-HT receptor blockade enhances Ca(2+)/calmodulin-dependent protein kinase II function and membrane expression of AMPA receptor subunits in the rat hippocampus: implications for memory formation.
    Schiapparelli L, Del Río J, Frechilla D.
    J Neurochem; 2005 Aug 15; 94(4):884-95. PubMed ID: 16092936
    [Abstract] [Full Text] [Related]

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