STUDIES REGARDING THE NEUROTOXIN 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE

关于神经毒素 1-甲基-4-苯基-1,2,3,6-四氢吡啶的研究

• 批准号: 3964164
• 负责人: A BROSSI
• 金额: --
• 依托单位: NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3964164
• 关键词: MAO inhibitors; Parkinson's disease; analgesics; antiadrenergic agents; biotransformation; brain metabolism; chemical structure function; chemical synthesis; dopamine; ferroxidase; neurotoxins; oxidation; piperidine; pyridine; pyridinones; toxin metabolism

MPTP is a pseudosubstrate for the copper oxidase ceruloplasmin, and both MPDP+ and MPP+ are produced. Incubation of MPTP with horseradish peroxidase only provided MPTP N-oxide. Oxidation of MPDP+ and MPP+ with potassium ferricyanide afforded a dihydropyridone and a pyridone respectively. MPTP analogs derived from prodine-type analgesics were found to be devoid of neurotoxic properties. A series of deuterated MPTP-analogs was prepared and their inhibitory effects on MAO B measured.

MPTP是铜氧化酶铜蓝蛋白的假底物， 产生MPDP+和MPP+。 用辣根孵育MPTP 过氧化物酶只提供MPTP N-氧化物。 MPDP+和MPP+的氧化 铁氰化钾得到二氢吡啶酮和吡啶酮 分别 发现了来自脯氨酸型镇痛药的MPTP类似物 没有神经毒性 一系列氘代MPTP类似物 并测定了它们对单胺氧化酶B的抑制作用。