Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
ACS Med Chem Lett
; 4(1): 46-51, 2013 Jan 10.
Article
en En
| MEDLINE
| ID: mdl-24900562
ABSTRACT
Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, along with nomifensine were tested in a rodent receptor occupancy study and demonstrated dose-dependent displacement of radiolabeled NET and DAT ligands. These compounds were efficacious in a rat forced swim assay (model of depression) and also had activity in rat spontaneous locomotion assay.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estados Unidos