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 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.
D000700:Analgesics / Q000138:chemical synthesis; D000818:Animals; D008722:Methods; D051379:Mice; D009281:Naphthalenes / Q000138:chemical synthesis*; D009292:Narcotic Antagonists / Q000138:chemical synthesis*; D009294:Narcotics / Q000138:chemical synthesis*; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
D000700:Analgesics; D009281:Naphthalenes; D009292:Narcotic Antagonists; D009294:Narcotics; D013764:Tetrahydronaphthalenes