Trubitsyna T K, Kashkovskiĭ M D
Farmakol Toksikol. 1980 Sep-Oct;43(5):530-6.
Pharmacological activity of the indolylalkyl derivatives of quipazin has been studied. 1-3(-Indolylmethyl)-4-(2"-quinolyl) piperazine dimaleate has proved to be the most active according to the tests used for examining the properties of quipazin. Like quipazin, it produces the contracture of smooth muscle organs and bronchospasm. It has a constrictive effect of the vessels, elicits central serotonin-positive actions, reduces the effect of reserpine and tetrabenazine, potentiates the central effects of amphetamine and L-DOPA. The drug does not affect the convulsant action of tryptamine in rats. Unlike imipramine, it shows no cholinolytic activity. Elongation of the methylene chain that connects the indole residue and the quipazin molecule leads to a decrease in the pharmacological activity.
已对喹哌嗪的吲哚烷基衍生物的药理活性进行了研究。根据用于检测喹哌嗪性质的试验，1-3(-吲哚甲基)-4-(2"-喹啉基)哌嗪二马来酸盐被证明是活性最强的。与喹哌嗪一样，它会引起平滑肌器官挛缩和支气管痉挛。它对血管有收缩作用，引发中枢5-羟色胺阳性作用，降低利血平和丁苯那嗪的作用，增强苯丙胺和左旋多巴的中枢作用。该药物不影响色胺在大鼠中的惊厥作用。与丙咪嗪不同，它没有抗胆碱活性。连接吲哚残基和喹哌嗪分子的亚甲基链的延长会导致药理活性降低。
