Mashkovsky M D, Andreyeva N I
Ann Ist Super Sanita. 1978;14(1):43-8.
During the search for new psychotropic drugs, a group of pyrazinoindole derivatives have been synthetized at the All Union Chemical Pharmaceutical Research Institute. Especially effective and having antidepressant activities is the hydrochloride of 1,10-trimethylene-8-methyl-1,2,3,4-tetrahydropyrazino (1,2-a) indole, named pyrazidol. Pyrazidol differs from any already known antidepressant for its chemical structure, the general pattern of activity and its neurochemical mechanism of action. The drug combines an inhibiting action on the neuronal uptake of monoamines with a monoamineoxidase inhibiting activity. As MAO-inhibitor, pyrazidol mainly impairs serotonin deamination, and acts only slightly on tyramine deamination. Furthermore, the anti-MAO action of pyrazidol is of short duration. Then, pyrazidol constitutes a drug with a particular profile of therapeutic activity.
在寻找新型精神药物的过程中,全苏化学制药研究所合成了一组吡嗪吲哚衍生物。1,10 - 三亚甲基 - 8 - 甲基 - 1,2,3,4 - 四氢吡嗪并(1,2 - a)吲哚的盐酸盐,即吡嗪醇,尤其有效且具有抗抑郁活性。吡嗪醇在化学结构、一般活性模式及其神经化学作用机制方面与任何已知的抗抑郁药都不同。该药物兼具对单胺类神经元摄取的抑制作用和单胺氧化酶抑制活性。作为单胺氧化酶抑制剂,吡嗪醇主要损害5 - 羟色胺脱氨基作用,对酪胺脱氨基作用影响较小。此外,吡嗪醇的抗单胺氧化酶作用持续时间较短。因此,吡嗪醇是一种具有特殊治疗活性特征的药物。