BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

127 related articles for article (PubMed ID: 20590088)

  • 1. Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
    Bromidge SM; Arban R; Bertani B; Bison S; Borriello M; Cavanni P; Dal Forno G; Di-Fabio R; Donati D; Fontana S; Gianotti M; Gordon LJ; Granci E; Leslie CP; Moccia L; Pasquarello A; Sartori I; Sava A; Watson JM; Worby A; Zonzini L; Zucchelli V
    J Med Chem; 2010 Aug; 53(15):5827-43. PubMed ID: 20590088
    [TBL] [Abstract][Full Text] [Related]  

  • 2. 8-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors--part II.
    Bromidge SM; Bertani B; Borriello M; Bozzoli A; Faedo S; Gianotti M; Gordon LJ; Hill M; Zucchelli V; Watson JM; Zonzini L
    Bioorg Med Chem Lett; 2009 Apr; 19(8):2338-42. PubMed ID: 19286377
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Simultaneous blockade of 5-HT1A/B receptors and 5-HT transporters results in acute increases in extracellular 5-HT in both rats and guinea pigs: in vivo characterization of the novel 5-HT1A/B receptor antagonist/5-HT transport inhibitor SB-649915-B.
    Hughes ZA; Starr KR; Scott CM; Newson MJ; Sharp T; Watson JM; Hagan JJ; Dawson LA
    Psychopharmacology (Berl); 2007 May; 192(1):121-33. PubMed ID: 17265079
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Characterization of the potent 5-HT(1A/B) receptor antagonist and serotonin reuptake inhibitor SB-649915: preclinical evidence for hastened onset of antidepressant/anxiolytic efficacy.
    Watson JM; Dawson LA
    CNS Drug Rev; 2007; 13(2):206-23. PubMed ID: 17627673
    [TBL] [Abstract][Full Text] [Related]  

  • 5. 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; Fletcher H; McGaughey G; Patel U; Webb MB; Yardley J; Andree T; Boast C; Kucharik RJ; Marquis K; Morris H; Scerni R; Moyer JA
    J Med Chem; 1999 Dec; 42(25):5077-94. PubMed ID: 10602693
    [TBL] [Abstract][Full Text] [Related]  

  • 6. De novo design of a picomolar nonbasic 5-HT(1B) receptor antagonist.
    Nugiel DA; Krumrine JR; Hill DC; Damewood JR; Bernstein PR; Sobotka-Briner CD; Liu J; Zacco A; Pierson ME
    J Med Chem; 2010 Feb; 53(4):1876-80. PubMed ID: 20088516
    [TBL] [Abstract][Full Text] [Related]  

  • 7. 3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors.
    Lovell PJ; Blaney FE; Goodacre CJ; Scott CM; Smith PW; Starr KR; Thewlis KM; Vong AK; Ward SE; Watson JM
    Bioorg Med Chem Lett; 2007 Feb; 17(4):1033-6. PubMed ID: 17129726
    [TBL] [Abstract][Full Text] [Related]  

  • 8. 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
    Bioorg Med Chem Lett; 2006 Mar; 16(5):1338-41. PubMed ID: 16332439
    [TBL] [Abstract][Full Text] [Related]  

  • 9. 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; 54(19):6657-69. PubMed ID: 21859099
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Novel mannich bases, 5-arylimidazolidine-2,4-dione derivatives with dual 5-HT(1A) receptor and serotonin transporter affinity.
    Czopek A; Kołaczkowski M; Bucki A; Byrtus H; Pawłowski M; Siwek A; Bojarski AJ; Bednarski M; Wróbel D; Wesołowska A
    Arch Pharm (Weinheim); 2013 Feb; 346(2):98-109. PubMed ID: 23288448
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Preclinical pharmacology and pharmacokinetics of AZD3783, a selective 5-hydroxytryptamine 1B receptor antagonist.
    Zhang M; Zhou D; Wang Y; Maier DL; Widzowski DV; Sobotka-Briner CD; Brockel BJ; Potts WM; Shenvi AB; Bernstein PR; Pierson ME
    J Pharmacol Exp Ther; 2011 Nov; 339(2):567-78. PubMed ID: 21825000
    [TBL] [Abstract][Full Text] [Related]  

  • 12. In vivo occupancy of the 5-HT1A receptor by a novel pan 5-HT1(A/B/D) receptor antagonist, GSK588045, using positron emission tomography.
    Comley RA; van der Aart J; Gulyás B; Garnier M; Iavarone L; Halldin C; Rabiner EA
    Neuropharmacology; 2015 May; 92():44-8. PubMed ID: 25476970
    [TBL] [Abstract][Full Text] [Related]  

  • 13. 3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
    Atkinson PJ; Bromidge SM; Duxon MS; Gaster LM; Hadley MS; Hammond B; Johnson CN; Middlemiss DN; North SE; Price GW; Rami HK; Riley GJ; Scott CM; Shaw TE; Starr KR; Stemp G; Thewlis KM; Thomas DR; Thompson M; Vong AK; Watson JM
    Bioorg Med Chem Lett; 2005 Feb; 15(3):737-41. PubMed ID: 15664848
    [TBL] [Abstract][Full Text] [Related]  

  • 14. 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.
    Procopiou PA; Ancliff RA; Bamford MJ; Browning C; Connor H; Davies S; Fogden YC; Hodgson ST; Holmes DS; Looker BE; Morriss KM; Parr CA; Pickup EA; Sehmi SS; White GV; Watts CJ; Wilson DM; Woodrow MD
    J Med Chem; 2007 Dec; 50(26):6706-17. PubMed ID: 18052318
    [TBL] [Abstract][Full Text] [Related]  

  • 15. An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
    Becker OM; Dhanoa DS; Marantz Y; Chen D; Shacham S; Cheruku S; Heifetz A; Mohanty P; Fichman M; Sharadendu A; Nudelman R; Kauffman M; Noiman S
    J Med Chem; 2006 Jun; 49(11):3116-35. PubMed ID: 16722631
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.
    Furlotti G; Alisi MA; Apicella C; Capezzone de Joannon A; Cazzolla N; Costi R; Cuzzucoli Crucitti G; Garrone B; Iacovo A; Magarò G; Mangano G; Miele G; Ombrato R; Pescatori L; Polenzani L; Rosi F; Vitiello M; Di Santo R
    J Med Chem; 2012 Nov; 55(22):9446-66. PubMed ID: 23043420
    [TBL] [Abstract][Full Text] [Related]  

  • 17. N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract.
    Leonardi A; Guarneri L; Poggesi E; Angelico P; Velasco C; Cilia A; Testa R
    J Pharmacol Exp Ther; 2001 Dec; 299(3):1027-37. PubMed ID: 11714892
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): in vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity.
    Dawson LA; Hughes ZA; Starr KR; Storey JD; Bettelini L; Bacchi F; Arban R; Poffe A; Melotto S; Hagan JJ; Price GW
    Neuropharmacology; 2006 Jun; 50(8):975-83. PubMed ID: 16581092
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
    Leslie CP; Biagetti M; Bison S; Bromidge SM; Di Fabio R; Donati D; Falchi A; Garnier MJ; Jaxa-Chamiec A; Manchee G; Merlo G; Pizzi DA; Stasi LP; Tibasco J; Vong A; Ward SE; Zonzini L
    J Med Chem; 2010 Dec; 53(23):8228-40. PubMed ID: 21053897
    [TBL] [Abstract][Full Text] [Related]  

  • 20. 2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.
    Zhou D; Gross JL; Adedoyin AB; Aschmies SB; Brennan J; Bowlby M; Di L; Kubek K; Platt BJ; Wang Z; Zhang G; Brandon N; Comery TA; Robichaud AJ
    J Med Chem; 2012 Mar; 55(5):2452-68. PubMed ID: 22313242
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 7.