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Pregled bibliografske jedinice broj: 607063

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

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 (međunarodna recenzija, članak, znanstveni)

CROSBI ID: 607063 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

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

Autori
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

Izvornik
Journal of medicinal chemistry (0022-2623) 53 (2010), 13; 4989-5001

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

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

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biologija, Temeljne medicinske znanosti



POVEZANOST RADA

Profili:

Avatar Url Maja Roščić (autor)

Poveznice na cjeloviti tekst rada:

doi pubs.acs.org pubs.acs.org

Citiraj ovu publikaciju:

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 (međunarodna recenzija, članak, znanstveni)
Micheli, F., Cavanni, P., Andreotti, D., Arban, R., Benedetti, R., Bertani, B., Bettati, M., Bettelini, L., Bonanomi, G. & Braggio, S. (2010) 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 (13), 4989-5001 doi:10.1021/jm100481d.
@article{article, author = {Micheli, Fabrizio and Cavanni, Paolo and Andreotti, Daniele and Arban, Roberto and Benedetti, Roberto and Bertani, Barbara and Bettati, Michela and Bettelini, Letizia and Bonanomi, Giorgio and Braggio, Simone and Carletti, Renzo and Checchia, Anna and Corsi, Mauro and Fazzolari, Elettra and Fontana, Stefano and Marchioro, Carla and Merlo-Pich, Emilio and Negri, Michele and Oliosi, Beatrice and Ratti, Emiliangelo and Read, Kevin D. and Ro\v{s}\v{c}i\'{c}, Maja and Sartori, Ilaria and Spada, Simone and Tedesco, Giovanna and Tarsi, Luca and Terreni, Silvia and Visentini, Filippo and Zocchi, Alessandro and Zonzini, Laura and Di Fabio, Romano}, year = {2010}, pages = {4989-5001}, DOI = {10.1021/jm100481d}, keywords = {CNS, depression, triple reuptake inhibitors, TRUI, monoamine transporters}, journal = {Journal of medicinal chemistry}, doi = {10.1021/jm100481d}, volume = {53}, number = {13}, issn = {0022-2623}, title = {6-(3, 4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor}, keyword = {CNS, depression, triple reuptake inhibitors, TRUI, monoamine transporters} }
@article{article, author = {Micheli, Fabrizio and Cavanni, Paolo and Andreotti, Daniele and Arban, Roberto and Benedetti, Roberto and Bertani, Barbara and Bettati, Michela and Bettelini, Letizia and Bonanomi, Giorgio and Braggio, Simone and Carletti, Renzo and Checchia, Anna and Corsi, Mauro and Fazzolari, Elettra and Fontana, Stefano and Marchioro, Carla and Merlo-Pich, Emilio and Negri, Michele and Oliosi, Beatrice and Ratti, Emiliangelo and Read, Kevin D. and Ro\v{s}\v{c}i\'{c}, Maja and Sartori, Ilaria and Spada, Simone and Tedesco, Giovanna and Tarsi, Luca and Terreni, Silvia and Visentini, Filippo and Zocchi, Alessandro and Zonzini, Laura and Di Fabio, Romano}, year = {2010}, pages = {4989-5001}, DOI = {10.1021/jm100481d}, keywords = {CNS, depression, triple reuptake inhibitors, TRUI, monoamine transporters}, journal = {Journal of medicinal chemistry}, doi = {10.1021/jm100481d}, volume = {53}, number = {13}, issn = {0022-2623}, title = {6-(3, 4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor}, keyword = {CNS, depression, triple reuptake inhibitors, TRUI, monoamine transporters} }

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE

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