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6-(3, 4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor (CROSBI ID 188280)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Micheli, Fabrizio ; Cavanni, Paolo ; Andreotti, Daniele ; Arban, Roberto ; Benedetti, Roberto ; Bertani, Barbara ; Bettati, Michela ; Bettelini, Letizia ; Bonanomi, Giorgio ; Braggio, Simone et al. 6-(3, 4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor // Journal of medicinal chemistry, 53 (2010), 13; 4989-5001. doi: 10.1021/jm100481d

Podaci o odgovornosti

Micheli, Fabrizio ; Cavanni, Paolo ; Andreotti, Daniele ; Arban, Roberto ; Benedetti, Roberto ; Bertani, Barbara ; Bettati, Michela ; Bettelini, Letizia ; Bonanomi, Giorgio ; Braggio, Simone ; Carletti, Renzo ; Checchia, Anna ; Corsi, Mauro ; Fazzolari, Elettra ; Fontana, Stefano ; Marchioro, Carla ; Merlo-Pich, Emilio ; Negri, Michele ; Oliosi, Beatrice ; Ratti, Emiliangelo ; Read, Kevin D. ; Roščić, Maja ; Sartori, Ilaria ; Spada, Simone ; Tedesco, Giovanna ; Tarsi, Luca ; Terreni, Silvia ; Visentini, Filippo ; Zocchi, Alessandro ; Zonzini, Laura ; Di Fabio, Romano

engleski

6-(3, 4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor

A pharmacophore model for triple reuptake inhibitors and the new class of 1-(aryl)-6-[alkoxyalkyl]-3- azabicyclo[3.1.0]hexanes were recently reported. Further investigation in this area led to the identification of a new series of potent and selective triple reuptake inhibitors endowed with good developability characteristics. Excellent bioavailability and brain penetration are associated with this series of 6-(3, 4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptanes together with high in vitro potency and selectivity at SERT, NET, and DAT. In vivo microdialysis experiments in different animal models and receptor occupancy studies in rat confirmed that derivative 17 showed an appropriate profile to guarantee further progression of the compound.

CNS; depression; triple reuptake inhibitors; TRUI; monoamine transporters

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Podaci o izdanju

53 (13)

2010.

4989-5001

objavljeno

0022-2623

10.1021/jm100481d

Povezanost rada

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Kemija, Temeljne medicinske znanosti, Biologija

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