The effect on ephedrine prodrugs on locomotor activity in rats

被引：16

作者：

Walker, RB

Fitz, LD

Williams, LM

McDaniel, YM

机构：

[1] Chemistry Department, University of Arkansas at Pine Bluff, Pine Bluff

来源：

GENERAL PHARMACOLOGY | 1996年 / 27卷 / 01期

关键词：

D O I：

10.1016/0306-3623(95)00127-1

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. Five oxazolidines were synthesized by reaction of (-) ephedrine with formaldehyde, propionaldehyde, butyraldehyde, isobutyraldehyde, and acetone, respectively. 2. Half-lives of hydrolysis were measured in pH 7.4 aqueous buffer. Half-lives varied from 12 seconds to 11 minutes. 3. The compounds were evaluated for their ability to increase locomotor activity in rats. All compounds significantly increased locomotor activity at 50 mg/kg dose. 4. The formaldehyde derivative had similar activity to (-) ephedrine. All other compounds were less active than (-) ephedrine.

引用

页码：109 / 111

页数：3

共 13 条

[1] CHIRAL 3-SUBSTITUTED ALDEHYDES - DETERMINATION OF ABSOLUTE-CONFIGURATIONS AND ENANTIOMERIC EXCESSES BY NMR ANALYSIS OF DERIVED OXAZOLIDINES [J].