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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: poffe a. 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
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: poffe a. 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
GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species.
Rutter AR, Poffe A, Cavallini P, Davis TG, Schneck J, Negri M, Vicentini E, Montanari D, Arban R, Gray FA, Davies CH, Wren PB. Rutter AR, et al. Among authors: poffe a. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. doi: 10.1124/jpet.114.214155. Epub 2014 Apr 30. J Pharmacol Exp Ther. 2014. PMID: 24784567
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: poffe a. Neuropharmacology. 2006 Jun;50(8):975-83. doi: 10.1016/j.neuropharm.2006.01.010. Epub 2006 Mar 31. Neuropharmacology. 2006. PMID: 16581092