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

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.