Abstract—We studied the effect of novel domestic derivatives of 3-oxypyridine and succinic acid (emoxypine, reamberin, and mexidol) on the activity of monoamine oxidases (MAO-A and MAO-B) and the level of biogenic amines (serotonin and dopamine) in the hypothalamus during the first two weeks of alloxan-induced diabetes in rats. During the first 14 days of alloxan-induced diabetes in rats, the levels of serotonin and dopamine decreased in the hypothalamus in the presence of unchanged MAO-B activity. The MAO-A activity and serotonin level in the hypothalamus of diabetic rats did not differ from the control values ​​at the initial stage of the experiment, and after a significant transient decrease, they again reached normal levels. The dopamine level in the hypothalamus of rats with experimental diabetes decreased only at the end of the experiment. The application of the studied drugs at doses equivalent to the therapeutic range for humans corrected the transient shifts in MAO-A activity and the delayed deficiency of monoamines in the hypothalamus of animals with alloxan-induced diabetes. The seven-day administration of an isolated derivative of 3-oxypyridine (emoxypine) and an isolated derivative of succinic acid (reamberin) prevented the transient decrease in MAO-A activity, compensated the concomitant deficiency of serotonin and increased the dopamine level in the hypothalamus of rats with alloxan-induced diabetes. Mexidol, which is simultaneously a derivative of 3‑oxypyridine and succinic acid, prevented a decrease in the hypothalamic levels of serotonin and dopamine in diabetic rats after 7 and 14-fold use (respectively). Correction of hypothalamic serotonin deficiency by Mexidol was not accompanied by changes in the activity of MAO-A and MAO-B. A decrease in hypothalamic dopamine deficiency as a result of a two-week administration of Mexidol was accompanied by a decrease in MAO-A activity. The intensity of neurochemical effects induced by derivatives of 3-oxypyridine and succinic acid were similar to α-lipoic acid which was used as a comparison drug.

中文翻译：

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3-氧吡啶衍生物和琥珀酸对四氧嘧啶糖尿病大鼠单胺氧化酶活性和下丘脑单胺含量的影响

摘要-我们研究了3-氧吡啶和琥珀酸的新型国产衍生物（奥克西平，reamberin和mexidol）对单胺氧化酶（MAO-A和MAO-B）活性以及生物胺（5-羟色胺和多巴胺）水平的影响在四氧嘧啶诱发的大鼠糖尿病的前两周中，下丘脑中的这种作用。在四氧嘧啶诱发的大鼠糖尿病的前14天中，在MAO-B活性不变的情况下，下丘脑中5-羟色胺和多巴胺的水平降低。糖尿病大鼠下丘脑中的MAO-A活性和血清素水平与实验初期的控制值没有差异，并且在短暂的显着下降后又恢复到正常水平。实验性糖尿病大鼠下丘脑中的多巴胺水平仅在实验结束时降低。所研究药物的剂量等于人类的治疗范围，从而纠正了四氧嘧啶诱发的糖尿病动物下丘脑中MAO-A活性的瞬时转变和单胺的延迟缺乏。服用7天的3-氧代吡啶（莫西平）的分离衍生物和琥珀酸（reamberin）的分离的衍生物预防了MAO-A活性的瞬时下降，补偿了血清素的同时缺乏，并增加了下丘脑中的多巴胺水平与四氧嘧啶诱发的糖尿病大鼠的关系。甲氧西多同时是3-氧吡啶和琥珀酸的衍生物，在分别使用7和14倍后，可防止糖尿病大鼠下丘脑中5-羟色胺和多巴胺的水平降低。通过美西多纠正下丘脑5-羟色胺缺乏症并没有伴随MAO-A和MAO-B活性的变化。服用美西多两周后导致下丘脑多巴胺缺乏症减少，同时MAO-A活性降低。3-氧吡啶和琥珀酸衍生物诱导的神经化学作用强度与用作比较药物的α-硫辛酸相似。