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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: gerrard p. 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
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. J Med Chem. 2009 May 28;52(10):3238-47. doi: 10.1021/jm900023b. J Med Chem. 2009. PMID: 19388677
Discovery and biological characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a new potent and selective neurokinin 1 (NK1) receptor antagonist clinical candidate.
Di Fabio R, Alvaro G, Griffante C, Pizzi DA, Donati D, Mattioli M, Cimarosti Z, Guercio G, Marchioro C, Provera S, Zonzini L, Montanari D, Melotto S, Gerrard PA, Trist DG, Ratti E, Corsi M. Di Fabio R, et al. J Med Chem. 2011 Feb 24;54(4):1071-9. doi: 10.1021/jm1013264. Epub 2011 Jan 13. J Med Chem. 2011. PMID: 21229983
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. 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
Receptor distribution studies.
Carletti R, Tacconi S, Mugnaini M, Gerrard P. Carletti R, et al. Among authors: gerrard p. Curr Opin Pharmacol. 2017 Aug;35:94-100. doi: 10.1016/j.coph.2017.07.008. Epub 2017 Aug 10. Curr Opin Pharmacol. 2017. PMID: 28803835 Review.
Transient forebrain over-expression of CRF induces plasma corticosterone and mild behavioural changes in adult conditional CRF transgenic mice.
Vicentini E, Arban R, Angelici O, Maraia G, Perico M, Mugnaini M, Ugolini A, Large C, Domenici E, Gerrard P, Bortner D, Mansuy IM, Mangiarini L, Merlo-Pich E. Vicentini E, et al. Among authors: gerrard p. Pharmacol Biochem Behav. 2009 Jul;93(1):17-24. doi: 10.1016/j.pbb.2009.03.015. Epub 2009 Apr 7. Pharmacol Biochem Behav. 2009. PMID: 19358863
57 results