Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives
摘要:
The synthesis and the opiate agonist and antagonist activities of three derivatives of cis-2-[methyl(cyclopropanemethyl)amino]-1-phenyltetralin are reported. The compounds were obtained by synthetic modification from 2-amino-1-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.
Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives
作者:William G. Reifenrath、David S. Fries
DOI:10.1021/jm00188a017
日期:1979.2
The synthesis and the opiate agonist and antagonist activities of three derivatives of cis-2-[methyl(cyclopropanemethyl)amino]-1-phenyltetralin are reported. The compounds were obtained by synthetic modification from 2-amino-1-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.
REIFENRATH W. G.; FRIES D. S., J. MED. CHEM., 1979, 22, NO 2, 204-206