Azetidine derivatives of tricyclic antidepressant agents.
Tricyclic derivatives of azetidine were synthesized and screened for their potential antidepressant activity. The active series had the tricyclic ring attached to position 1 and a basic group in position 3 of the azetidine. The most interesting compounds were comparable to the reference standards for reserpine antagonism in mice, the most active being the dextrorotatory methylamino derivative 84. The pharmacological profile classifies it as a CNS stimulant devoid of peripheral anticholinergic activity.
D000818:Animals; D000927:Anticonvulsants; D000929:Antidepressive Agents, Tricyclic / Q000138:chemical synthesis*; D001384:Azetidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001385:Azetines / Q000138:chemical synthesis*; D001831:Body Temperature / Q000187:drug effects; D007928:Lethal Dose 50; D008297:Male; D008722:Methods; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D012110:Reserpine / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D000929:Antidepressive Agents, Tricyclic; D001384:Azetidines; D001385:Azetines; D012110:Reserpine; D010433:Pentylenetetrazole