Basic derivatives of 6,7-dihydroindolo(1,7-ab)(1) benzazepine and 6H-indolo(7,1-cd)(1,5) benzoxazepine as potential antidepressant agents.
Basic derivatives of 6,7-dihydroindolo[1,7-ab][1]benzazepine and 6H-indolo[7,1-cd][1,5]benzoxazepine incorporating the imipramine basic side chain were synthesized and screened for antidepressant activity in mice. With few exceptions, the compounds unsubstituted at C-2 antagonized reserpine-induced ptosis and hypothermia showing negligible anticholinergic and antihistaminic properties. The compound 1-[2-(N-methyl-N-benzylamino)ethyl]-6,7-dihydroindolo[1,7-ab][1]benzazepine had the highest toxicity-activity ratio.
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001763:Blepharoptosis / Q000517:prevention & control; D001831:Body Temperature / Q000187:drug effects; D003864:Depression, Chemical; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D012110:Reserpine / Q000037:antagonists & inhibitors
D000928:Antidepressive Agents; D001552:Benzazepines; D007211:Indoles; D012110:Reserpine