Analgesic and tranquilizing activity of 5,8-disubstituted 1-tetralone Mannich bases.
5,8-Disubstituted 1-tetralone Mannich bases represent semirigid variants of classical (i.e., chlorpromazine) neuroleptic agents. 8-Chloro-5-methoxy-2-morpholinomethyl-1-tetralone exhibits neuroleptic potency in the thiothixene range in animal models. Of greater potential interest, however, is the analgesic potency of the 8-chloro-5-methoxy-2-pyrrolidinomethyl analogue which was in the morphine range. This compound did not induce tolerance nor was its activity reversed by naloxone. Structure-activity relationships of the series are discussed.
D000661:Amphetamine / Q000037:antagonists & inhibitors; D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D001362:Avoidance Learning / Q000187:drug effects; D004285:Dogs; D006358:Hot Temperature; D008352:Mannich Bases / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D013216:Reflex, Startle / Q000187:drug effects; D013329:Structure-Activity Relationship; D014149:Tranquilizing Agents / Q000138:chemical synthesis*
D000700:Analgesics; D008352:Mannich Bases; D009281:Naphthalenes; D014149:Tranquilizing Agents; D000661:Amphetamine