SYNTHESES AND ANTICHOLINESTERASE ACTIVITY OF TETRAHYDROBENZAZEPINE CARBAMATES

被引：15

作者：

CHEN, YL ^{[1
]}

LISTON, D ^{[1
]}

NIELSEN, J ^{[1
]}

CHAPIN, D ^{[1
]}

DUNAISKIS, A ^{[1
]}

HEDBERG, K ^{[1
]}

IVES, J ^{[1
]}

JOHNSON, J ^{[1
]}

JONES, S ^{[1
]}

机构：

[1] PFIZER INC,DEPT NEUROSCI,DIV CENT RES,GROTON,CT 06340

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 13期

关键词：

D O I：

10.1021/jm00039a013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of a series of alkylcarbamates of 1,5-methano-2,3,4,5-tetrahydro-1H-2-benzazepin-7-ol is reported. Many of these compounds are potent acetylcholinesterase (AChE) inhibitors. The in vitro AChE inhibition, cholinergic effects, acute toxicity, and elevation of brain acetylcholine levels in vivo of this series of compounds are described, A representative compound, 1d (5,6 mg/kg, po), was able to reverse hemicolinium-3-induced amnesia in the mouse passive avoidance assay.

引用

页码：1996 / 2000

页数：5

共 8 条

[1] PHARMACOLOGICAL INVESTIGATIONS OF NEUROTRANSMITTER INVOLVEMENT IN PASSIVE-AVOIDANCE RESPONDING - A REVIEW AND SOME NEW RESULTS [J].