Artemenko G N, Vikhliaev Iu I, Kucherova N F, Borisova L N
Farmakol Toksikol. 1976 Nov-Dec;39(6):651-5.
The spectrum of the psychotropic activity of a number of new pyrimidoindole derivatives and the relation between their chemical structure and activity were studied experimentally. The research was done on mice by employing tests usually applied in estimating neuroleptics and antidepressants of tricyclic structure. The study of indole derivatives are shown to display a sedative action. 5-methyl derivatives of pyrimido- and tetrahydropyrimido [3,4-a] indole without any substituent in the 2nd position are 5-oxytryptophan antagonists. The 2,5-dimethyltetrahydropyrimido [3,4-a] indole derivatives electively potentiate the central effect of 5-oxytryptophan and display in experiments a specific spectrum of the pharmacological action, resembling antidepressants by a number of tests. As concerns their activity these compounds, however, are inferior to amitriptyline and pyrasidol.
对一些新的嘧啶并吲哚衍生物的精神活性谱及其化学结构与活性之间的关系进行了实验研究。该研究是在小鼠身上进行的，采用了通常用于评估三环结构抗精神病药和抗抑郁药的测试。研究表明吲哚衍生物具有镇静作用。嘧啶并[3,4-a]吲哚和四氢嘧啶并[3,4-a]吲哚的5-甲基衍生物在第2位没有任何取代基，它们是5-羟色氨酸拮抗剂。2,5-二甲基四氢嘧啶并[3,4-a]吲哚衍生物选择性地增强5-羟色氨酸的中枢作用，并在实验中显示出特定的药理作用谱，在许多测试中类似于抗抑郁药。然而，就其活性而言，这些化合物不如阿米替林和匹拉唑。
