AMINOTETRALINS AS NARCOTIC-ANTAGONISTS - SYNTHESIS AND OPIATE-RELATED ACTIVITY OF 1-PHENYL-2-AMINOTETRALIN DERIVATIVES

被引:11
作者
REIFENRATH, WG [1 ]
FRIES, DS [1 ]
机构
[1] UNIV PACIF,SCH PHARM,MED & BIOL CHEM UNIT,STOCKTON,CA 95211
关键词
D O I
10.1021/jm00188a017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and the opiate agonist and antagonist activities of three derivatives of ci&s-2-[methyl(cyclopropanemethyl)amino]-l-phenyltetralin are reported. The compounds were obtained by synthetic modification from 2-amino-l-tetralone. The 1-propionoxy derivative 4c shows analgetic activity (ED50= 17.8 mg/kg) one-half that of codeine, and the 1-methoxy derivative 4b has weak antagonist activity (AD50= 33.5 mg/kg). The compounds showed no other significant opiate-related activity. © 1979, American Chemical Society. All rights reserved.
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页码:204 / 206
页数:3
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