REVERSAL OF COGNITIVE IMPAIRMENT BY HEPTYL PHYSOSTIGMINE, A LONG-LASTING CHOLINESTERASE INHIBITOR, IN PRIMATES

被引：33

作者：

RUPNIAK, NMJ ^{[1
]}

TYE, SJ ^{[1
]}

BRAZELL, C ^{[1
]}

HEALD, A ^{[1
]}

IVERSEN, SD ^{[1
]}

PAGELLA, PG ^{[1
]}

机构：

[1] MEDIOLANUM FARMACEUT,RES LABS,MILAN,ITALY

来源：

JOURNAL OF THE NEUROLOGICAL SCIENCES | 1992年 / 107卷 / 02期

关键词：

ACETYLCHOLINE; SCOPOLAMINE; COGNITION; ALZHEIMERS DISEASE; PRIMATE;

D O I：

10.1016/0022-510X(92)90296-W

中图分类号：

R74 [神经病学与精神病学];

学科分类号：

摘要：

Cholinergic replacement therapy for Alzheimer's disease using existing cholinesterase inhibitors is compromised by short duration, meagre benefits restricted to subgroups of patients, and peripheral toxicity. Heptyl physostigmine is a lipophilic carbamate derivative of physostigmine. In rhesus monkeys, heptyl physostigmine (0.2-0.9 mg/kg i.m.) fully reversed a scopolamine-induced cognitive impairment. Following oral administration in squirrel monkeys, heptyl physostigmine (8 mg/kg) induced long-lasting hypothermia (greater-than-or-equal-to 4 h), a centrally-mediated cholinergic effect. Erythrocyte acetylcholinesterase activity was inhibited by 86% at the time of peak hypothermia (180 min). Clinical trials with heptyl physostigmine will enable a more rigorous evaluation of cholinomimetic therapy for dementia.

引用

页码：246 / 249

页数：4

共 15 条

[1] THE CHOLINERGIC HYPOTHESIS OF GERIATRIC MEMORY DYSFUNCTION [J].