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SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.
Thomas DR, Melotto S, Massagrande M, Gribble AD, Jeffrey P, Stevens AJ, Deeks NJ, Eddershaw PJ, Fenwick SH, Riley G, Stean T, Scott CM, Hill MJ, Middlemiss DN, Hagan JJ, Price GW, Forbes IT. Thomas DR, et al. Among authors: melotto s. Br J Pharmacol. 2003 Jun;139(4):705-14. doi: 10.1038/sj.bjp.0705290. Br J Pharmacol. 2003. PMID: 12812993 Free PMC article.
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. Dawson LA, et al. Among authors: melotto s. Neuropharmacology. 2006 Jun;50(8):975-83. doi: 10.1016/j.neuropharm.2006.01.010. Epub 2006 Mar 31. Neuropharmacology. 2006. PMID: 16581092
SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test.
Starr KR, Price GW, Watson JM, Atkinson PJ, Arban R, Melotto S, Dawson LA, Hagan JJ, Upton N, Duxon MS. Starr KR, et al. Among authors: melotto s. Neuropsychopharmacology. 2007 Oct;32(10):2163-72. doi: 10.1038/sj.npp.1301341. Epub 2007 Mar 14. Neuropsychopharmacology. 2007. PMID: 17356576
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Di Fabio R, Alvaro G, Braggio S, Carletti R, Gerrard PA, Griffante C, Marchioro C, Pozzan A, Melotto S, Poffe A, Piccoli L, Ratti E, Tranquillini E, Trower M, Spada S, Corsi M. Di Fabio R, et al. Among authors: melotto s. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. doi: 10.1016/j.bmc.2013.09.001. Epub 2013 Sep 11. Bioorg Med Chem. 2013. PMID: 24075145
Discovery process and pharmacological characterization of 2-(S)-(4-fluoro-2-methylphenyl)piperazine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethylphenyl)ethyl]methylamide (vestipitant) as a potent, selective, and orally active NK1 receptor antagonist.
Di Fabio R, Griffante C, Alvaro G, Pentassuglia G, Pizzi DA, Donati D, Rossi T, Guercio G, Mattioli M, Cimarosti Z, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. Among authors: melotto s. J Med Chem. 2009 May 28;52(10):3238-47. doi: 10.1021/jm900023b. J Med Chem. 2009. PMID: 19388677
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Sabbatini FM, Di Fabio R, Griffante C, Pentassuglia G, Zonzini L, Melotto S, Alvaro G, Capelli AM, Pippo L, Perdona' E, St Denis Y, Costa S, Corsi M. Sabbatini FM, et al. Among authors: melotto s. Bioorg Med Chem Lett. 2010 Jan 15;20(2):623-7. doi: 10.1016/j.bmcl.2009.11.078. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19963378
Discovery process and characterization of novel carbohydrazide derivatives as potent and selective GHSR1a antagonists.
Sabbatini FM, Di Fabio R, Corsi M, Cavanni P, Bromidge SM, St-Denis Y, D'Adamo L, Contini S, Rinaldi M, Guery S, Savoia C, Mundi C, Perini B, Carpenter AJ, Dal Forno G, Faggioni F, Tessari M, Pavone F, Di Francesco C, Buson A, Mattioli M, Perdona' E, Melotto S. Sabbatini FM, et al. Among authors: melotto s. ChemMedChem. 2010 Sep 3;5(9):1450-5. doi: 10.1002/cmdc.201000185. ChemMedChem. 2010. PMID: 20593439 No abstract available.
22 results