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