A compound with low toxicity and pronounced antidepressant activity upon single and long-term administration was discovered by us earlier among a series of new thietanylxanthine derivatives. The present article focused on the central mechanisms of action of 2-[3-methyl-7-(thietan-3-yl)-1-ethylxanth-7-ylthio]acetic acid hydrazide (laboratory code M-20). Neuropharmacological analysis showed that M-20 at doses of 0.97 and 12 mg/kg exhibited effects indicative of possible stimulatory action on adrenergic and inhibitory action on GABA-ergic neurotransmission in brains of outbred white mice. M-20 at a dose of 12 mg/kg produced an activating effect on the serotoninergic system in addition to action on the adrenergic and GABA-ergic systems and altered the activity of the cholinergic system. M-20 at doses of 0.97 and 12 mg/kg did not alter the effects of haloperidol and L-DOPA, which indicated that it did not influence dopaminergic neurotransmission and MAO-inhibiting activity. The results indicated that M-20 was promising (at the low dose) for use with depression associated with decreased activity of the serotoninergic system without side effects on the dopaminergic and cholinergic systems.

中文翻译：

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2-[3-Methyl-7-(Thietan-3-Yl)-1-Ethylxanth-8-YLTHIO]醋酸酰肼的抗抑郁作用的神经药理学分析

我们较早在一系列新的硫杂环丁烷黄嘌呤衍生物中发现了一种毒性低、单次和长期给药具有显着抗抑郁活性的化合物。本文重点介绍 2-[3-methyl-7-(thietan-3-yl)-1-ethylxanth-7-ylthio] 乙酸酰肼（实验室代码 M-20）的核心作用机制。神经药理学分析表明，0.97 和 12 mg/kg 剂量的 M-20 表现出的作用表明可能对远交白鼠大脑中的肾上腺素能有刺激作用和对 GABA 能神经传递有抑制作用。12 mg/kg 剂量的 M-20 除了对肾上腺素能和 GABA 能系统产生作用外，还对 5-羟色胺能系统产生激活作用，并改变胆碱能系统的活性。M-20 的剂量为 0。97 和 12 mg/kg 不会改变氟哌啶醇和左旋多巴的作用，这表明它不会影响多巴胺能神经传递和 MAO 抑制活性。结果表明，M-20（低剂量）有望用于治疗与血清素能系统活性降低相关的抑郁症，而不会对多巴胺能和胆碱能系统产生副作用。