[Role of magnesium ions on the regulation of NMDA receptor--a pharmacopathology of memantine].
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.
Kato
Takeshi
T
Yokohama City University Graduate School of Integrated Science, Laboratories of Molecular Recognition and Information Science.
D000544:Alzheimer Disease / Q000188:drug therapy; D001665:Binding Sites; D002545:Brain Ischemia / Q000517:prevention & control; D016291:Dizocilpine Maleate / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D008274:Magnesium / Q000378:metabolism / Q000494:pharmacology / Q000502:physiology* / Q000627:therapeutic use; D008559:Memantine / Q000378:metabolism / Q000494:pharmacology*; D010622:Phencyclidine / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012559:Schizophrenia / Q000139:chemically induced
D016194:Receptors, N-Methyl-D-Aspartate; D016291:Dizocilpine Maleate; D008274:Magnesium; D010622:Phencyclidine; D008559:Memantine