Grol C J, Westenberg G, Hazelhoff B, De Vries J
Pharm Weekbl Sci. 1983 Dec 16;5(6):329-32. doi: 10.1007/BF02074864.
The synthesis of the semi-rigid imipramine analogue 2-(N,N-dimethylaminomethylene)-2,3,7,8-tetrahydro-1H-quino[1,8-ab] [I]-benzazepine is described. The compound was pharmacologically evaluated in a number of general in vivo screening tests for antidepressive activity. From these preliminary tests the compound appeared to show an imipramine-like activity. However, it did not have an effect on the noradrenaline depletion by 4, alpha-dimethyl-m-tyramine. These results are discussed on the basis of the conformational requirements determining the pharmacological profile of antidepressants.
描述了半刚性丙咪嗪类似物2-(N,N-二甲基氨基亚甲基)-2,3,7,8-四氢-1H-喹诺[1,8-ab][1]-苯并氮杂䓬的合成。该化合物在多项一般性体内抗抑郁活性筛选试验中进行了药理学评估。从这些初步试验来看，该化合物似乎显示出类似丙咪嗪的活性。然而，它对4,α-二甲基间酪氨酸所致的去甲肾上腺素耗竭没有影响。根据决定抗抑郁药药理学特征的构象要求对这些结果进行了讨论。
