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首页> 外文期刊>CNS drug reviews >Mildronate: an antiischemic drug for neurological indications.
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Mildronate: an antiischemic drug for neurological indications.

机译：Mildronate：一种抗缺血药物，可用于神经系统适应症。

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Mildronate (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; meldonium, quaterine) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. Mildronate was designed to inhibit carnitine biosynthesis in order to prevent accumulation of cytotoxic intermediate products of fatty acid beta-oxidation in ischemic tissues and to block this highly oxygen-consuming process. Mildronate is efficient in the treatment of heart ischemia and its consequences. Extensive evaluation of pharmacological activities of mildronate revealed its beneficial effect on cerebral circulation disorders and central nervous system (CNS) functions. The drug is used in neurological clinics for the treatment of brain circulation disorders. It appears to improve patients' mood; they become more active, their motor dysfunction decreases, and asthenia, dizziness and nausea become less pronounced. Since the brain does not utilize fatty acids as fuel other mechanisms of action of mildronate in CNS should be considered. Several reports indicate the possible existence of an alternative, non-carnitine dependent mechanism of action of mildronate. Our recent findings suggest that CNS effects of mildronate could be mediated by stimulation of the nitric oxide production in the vascular endothelium by modification of the gamma-butyrobetaine and its esters pools. It is hypothesized that mildronate may increase the formation of the gamma-butyrobetaine esters. The latter are potent cholinomimetics and may activate eNOS via acetylcholine receptors or specific gamma-butyrobetaine ester receptors. This article summarizes known pharmacological effects of mildronate, its pharmacokinetics, toxicology, as well as the proposed mechanisms of action.
机译：Mildronate（3-（2,2,2-三甲基肼基）丙酸酯; MET-88; meldonium，quaterine）是拉脱维亚有机合成研究所开发的抗缺血药物。 Mildronate设计用于抑制肉碱的生物合成，以防止缺血性组织中脂肪酸β-氧化的细胞毒性中间产物的积累，并阻止这种高度耗氧的过程。米尔膦酸盐对心脏缺血及其后果有效。大量的药草酸药草活性评估表明其对脑循环疾病和中枢神经系统（CNS）功能具有有益作用。该药物在神经科诊所用于治疗脑循环疾病。它似乎可以改善患者的情绪;他们变得更加活跃，运动功能障碍减少，乏力，头晕和恶心变得不那么明显。由于大脑不利用脂肪酸作为燃料，因此应考虑中枢神经系统中丙二酸酯的其他作用机制。几份报告表明，可能存在替代的，非肉碱依赖性的吡ron酸作用机理。我们最近的发现表明，可以通过修饰γ-丁甜菜碱及其酯库来刺激血管内皮中一氧化氮的产生，从而介导亚硝酸盐对中枢神经系统的影响。据推测，丙二酸酯可增加γ-丁甜菜碱酯的形成。后者是有效的拟胆碱药物，可以通过乙酰胆碱受体或特定的γ-丁甜菜碱酯受体激活eNOS。本文总结了吡ron酸的已知药理作用，药代动力学，毒理学以及拟议的作用机理。

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