SYNTHESIS AND PHARMACOLOGIC CHARACTERIZATION OF AN ALKYLATING ANALOG (CHLORNALTREXAMINE) OF NALTREXONE WITH ULTRA-LONG-LASTING NARCOTIC-ANTAGONIST PROPERTIES

被引：136

作者：

PORTOGHESE, PS ^{[1
]}

LARSON, DL ^{[1
]}

JIANG, JB ^{[1
]}

CARUSO, TP ^{[1
]}

TAKEMORI, AE ^{[1
]}

机构：

[1] UNIV MINNESOTA, SCH MED, DEPT PHARMACOL, MINNEAPOLIS, MN 55455 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 02期

关键词：

D O I：

10.1021/jm00188a008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Chlornaltrexamine (CNA) produces ultralong-lasting (3-6 days) narcotic antagonism in mice and persistent stereospecific binding to rat-brain homogenate. Protection studies in mice suggest that CNA mediates its narcotic antagonist effects by interacting with the same receptors that are occupied by naloxone. A single intracerebrovascular dose of CNA inhibits the development of physical dependence on morphine in mice for at least 3 days. CNA apparently exerts its sustained effects by selective covalent association with opioid receptors.

引用

页码：168 / 173

页数：6

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