Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-1-aminotetralin derivatives

Publisher Website
Google Scholar
Abstract
The synthesis and the opiate agonist and antagonist activites of 3 derivatives of cis-2-[methyl(cyclopropanemethyl)amino]-1-phenyletralin are reported. The compounds were obtained by synthetic modification from 2-amino-1-tetralone. The 1-propionoxy derivative shows analgetic activity (ED50 = 17.8 mg/kg) 1/2 that of codeine, and the 1-methoxy derivative has weak antagonist activity (AD50 = 33.5 mg/kg) [in mice]. The compounds showed no other significant opiate-related activity.