SYNTHESIS AND EVALUATION OF THE ANTIDEPRESSANT ACTIVITY OF THE ENANTIOMERS OF BUPROPION

Authors
MUSSO DL MEHTA NB SOROKO FE FERRIS RM HOLLINGSWORTH EB KENNEY BT
Citation
Dl. Musso et al., SYNTHESIS AND EVALUATION OF THE ANTIDEPRESSANT ACTIVITY OF THE ENANTIOMERS OF BUPROPION, Chirality, 5(7), 1993, pp. 495-500
Citations number
12
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Chirality → ACNP
ISSN journal
08990042
Volume
5
Issue
7
Year of publication
1993
Pages
495 - 500
Database
ISI
SICI code
0899-0042(1993)5:7<495:SAEOTA>2.0.ZU;2-G
Abstract
The synthesis of the enantiomers of bupropion, (rac)-2-tert-butylamino -3'-chloropropiophenone 1 (Wellbutrin(R)) is described. The enantiomer s were compared with the racemate in both the tetrabenazine-induced se dation model and the inhibition of uptake of biogenic amine assay. No significant differences were found in their potencies to reverse tetra benazine-induced sedation in mice or in their IC50 values as inhibitor s of biogenic amine uptake into nerve endings obtained from mouse brai n. (C) 1993 Wiley-Liss, Inc.