10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents.
An investigation of the structural requirements for CNS activity of the title compounds was undertaken. A synthesis of the precursor dihydro-10H-thieno[3,4-b][1,5]benzodiazepin-10-ones was achieved and three routes for their conversion to the title compounds were developed. The compounds were tested for neuroleptic activity by means of the blockade or d-amphetamine lethality in aggregated mice and/or effects on locomotor activity in rats. Antidepressant activity was examined using inhibition of tetrabenazine-induced depression in mice. Most of the compounds were found to be potent neuroleptic agents with several exhibiting additional antidepressant activity.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis*; D014150:Antipsychotic Agents / Q000138:chemical synthesis*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002375:Catalepsy / Q000139:chemically induced; D003913:Dextroamphetamine / Q000037:antagonists & inhibitors / Q000633:toxicity; D005106:Exploratory Behavior / Q000187:drug effects; D006801:Humans; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship; D013747:Tetrabenazine / Q000037:antagonists & inhibitors
D014151:Anti-Anxiety Agents; D014150:Antipsychotic Agents; D001569:Benzodiazepines; D003913:Dextroamphetamine; D013747:Tetrabenazine