Kato Takeshi
Yokohama City University Graduate School of Integrated Science, Laboratories of Molecular Recognition and Information Science.
Clin Calcium. 2004 Aug;14(8):76-80.
Magnesium ion blocks the ion channel of the NMDA receptor at a stable condition. The ion channel competes with the binding site of the noncompetitive antagonists phencyclidine (PCP) and MK-801, which prevent a brain impairment due to the ischemia and so on. The binding ability of these antagonists is strong, an exchange with the magnesium ion is not easy, then the side effect of the schizophrenia-like behavior is caused. Recently, memantine can be used as a therapeutic drug of the moderate-to-severe Alzheimer's disease. Memantine is the noncompetitive antagonist, too, then those development details and a difference from MK-801 were explained.
镁离子在稳定状态下阻断NMDA受体的离子通道。该离子通道与非竞争性拮抗剂苯环己哌啶(PCP)和MK-801的结合位点竞争,这些拮抗剂可预防因缺血等导致的脑损伤。这些拮抗剂的结合能力很强,不易与镁离子交换,进而导致精神分裂症样行为的副作用。最近,美金刚可作为中重度阿尔茨海默病的治疗药物。美金刚也是非竞争性拮抗剂,随后对其研发细节及与MK-801的差异进行了解释。