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

被引：34

作者：

MUSSO, DL ^{[1
]}

MEHTA, NB ^{[1
]}

SOROKO, FE ^{[1
]}

FERRIS, RM ^{[1
]}

HOLLINGSWORTH, EB ^{[1
]}

KENNEY, BT ^{[1
]}

机构：

[1] BURROUGHS WELLCOME CO,DEPT PHARMACOL,RES TRIANGLE PK,NC 27709

来源：

CHIRALITY | 1993年 / 5卷 / 07期

关键词：

DIBORANE AND SODIUM BOROHYDRIDE REDUCTION; DIASTEREOMERIC AMINO ALCOHOLS; SWERN OXIDATION; ANTITETRABENAZINE ACTIVITY; BIOGENIC AMINE UPTAKE INHIBITION;

D O I：

10.1002/chir.530050704

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of the enantiomers of bupropion, (rac)-2-tert-butylamino-3'-chloropropiophenone 1 (Wellbutrin(R)) is described. The enantiomers were compared with the racemate in both the tetrabenazine-induced sedation model and the inhibition of uptake of biogenic amine assay. No significant differences were found in their potencies to reverse tetrabenazine-induced sedation in mice or in their IC50 values as inhibitors of biogenic amine uptake into nerve endings obtained from mouse brain. (C) 1993 Wiley-Liss, Inc.

引用

页码：495 / 500

页数：6

共 12 条

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