Melloni P, Della Torre A, Meroni M, Ambrosini A, Rossi A C
J Med Chem. 1979 Feb;22(2):183-91. doi: 10.1021/jm00188a012.
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.
合成了氮杂环丁烷的三环衍生物，并对其潜在的抗抑郁活性进行了筛选。活性系列中，三环与氮杂环丁烷的1位相连，碱性基团位于3位。最有趣的化合物在小鼠体内对利血平拮抗作用方面可与参比标准品相媲美，其中活性最强的是右旋甲基氨基衍生物84。其药理特性将它归类为一种没有外周抗胆碱能活性的中枢神经系统兴奋剂。
