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Page 1
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M. Di Fabio R, et al. Among authors: piccoli l. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21831639
Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.
Gianotti M, Botta M, Brough S, Carletti R, Castiglioni E, Corti C, Dal-Cin M, Delle Fratte S, Korajac D, Lovric M, Merlo G, Mesic M, Pavone F, Piccoli L, Rast S, Roscic M, Sava A, Smehil M, Stasi L, Togninelli A, Wigglesworth MJ. Gianotti M, et al. Among authors: piccoli l. J Med Chem. 2010 Nov 11;53(21):7778-95. doi: 10.1021/jm100856p. J Med Chem. 2010. PMID: 20942472
rKv1.2 overexpression in the central medial thalamic area decreases caffeine-induced arousal.
Cazzin C, Piccoli L, Massagrande M, Garbati N, Michielin F, Knaus HG, Ring CJ, Morrison AD, Merlo-Pich E, Rovo Z, Astori S, Lüthi A, Corti C, Corsi M. Cazzin C, et al. Among authors: piccoli l. Genes Brain Behav. 2011 Nov;10(8):817-27. doi: 10.1111/j.1601-183X.2011.00719.x. Epub 2011 Aug 7. Genes Brain Behav. 2011. PMID: 21762462 Free article.
Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats.
Piccoli L, Micioni Di Bonaventura MV, Cifani C, Costantini VJ, Massagrande M, Montanari D, Martinelli P, Antolini M, Ciccocioppo R, Massi M, Merlo-Pich E, Di Fabio R, Corsi M. Piccoli L, et al. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011. doi: 10.1038/npp.2012.48. Epub 2012 May 9. Neuropsychopharmacology. 2012. PMID: 22569505 Free PMC article.
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: piccoli l. 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
The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.
Sabat M, Raveglia LF, Aldegheri L, Barilli A, Bianchi F, Brault L, Brodbeck D, Feriani A, Lingard I, Miura J, Myers R, Piccoli L, Tassini S, Tyhonas J, Ton-Nu T, Wang H, Virginio C. Sabat M, et al. Among authors: piccoli l. Bioorg Med Chem. 2022 Dec 15;76:117084. doi: 10.1016/j.bmc.2022.117084. Epub 2022 Nov 6. Bioorg Med Chem. 2022. PMID: 36402081
From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents.
Barilli A, Aldegheri L, Bianchi F, Brault L, Brodbeck D, Castelletti L, Feriani A, Lingard I, Myers R, Nola S, Piccoli L, Pompilio D, Raveglia LF, Salvagno C, Tassini S, Virginio C, Sabat M. Barilli A, et al. Among authors: piccoli l. J Med Chem. 2021 May 13;64(9):5931-5955. doi: 10.1021/acs.jmedchem.1c00065. Epub 2021 Apr 23. J Med Chem. 2021. PMID: 33890770
A novel process driving Alzheimer's disease validated in a mouse model: Therapeutic potential.
Greenfield SA, Cole GM, Coen CW, Frautschy S, Singh RP, Mekkittikul M, Garcia-Ratés S, Morrill P, Hollings O, Passmore M, Hasan S, Carty N, Bison S, Piccoli L, Carletti R, Tacconi S, Chalidou A, Pedercini M, Kroecher T, Astner H, Gerrard PA. Greenfield SA, et al. Among authors: piccoli l. Alzheimers Dement (N Y). 2022 Apr 5;8(1):e12274. doi: 10.1002/trc2.12274. eCollection 2022. Alzheimers Dement (N Y). 2022. PMID: 35415206 Free PMC article.
123 results