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: 4689175
• 负责人: A BROSSI
• 金额: --
• 依托单位: NAT INST OF ARTHRITIS, DIABETES, DIGESTIVE & 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/4689175
• 关键词: MAO inhibitors; antiadrenergic agents; biotransformation; brain metabolism; chemical structure function; chemical synthesis; dopamine; neurotoxins; piperidine; pyridine; toxin metabolism

MPDP+ has been recognized to be an intermediary metabolite in the conversion of MPTP into MPP+. MPDP+ disproportionates at physiological pH into MPTP and MPP+. MPTP, MPDP+ and MPP+ are inhibitors of monoamineoxidase B, and all three inhibit dopamine uptake in rat synaptosomal preparations. New synthesis of MPDP+ were developed and analogs of MPTP with the phenyl group at different positions of the tetrahydropyridine ring, and with N-alkyl groups instead of an N-methyl group were prepared. The biological effects demonstrated by MPTP were not shown by any of its analogs prepared thus far.

MPDP+已被认为是代谢物中的中间代谢物。 将MPTP转换为MPP+。 MPDP+在生理pH下水解 MPTP和MPP+。 MPTP、MPDP+和MPP+是 单胺氧化酶B，并且所有三种都抑制大鼠多巴胺摄取 突触体制备。 开发了MPDP+的新合成方法， 在MPTP的不同位置具有苯基的MPTP类似物 四氢吡啶环，并且用N-烷基代替N-甲基 组准备。 MPTP所显示的生物学效应并不 迄今为止制备的任何类似物都显示出了这一点。