[Memantine: a therapeutic drug for Alzheimer's disease and the comparison with MK-801].
Memantine is agreed officially as a therapeutic drug for moderate-to-severe Alzheimer's disease (AD) in EU and USA. Memantine is a similar uncompetitive NMDA-receptor antagonist to MK-801 and phencyclidine (PCP), and it prevents nerve cell death induced by the ischemia which induces as excessive release of glutamate. These medicines act on an ion channel binding site similar to the magnesium ion binding site. However, MK-801 and PCP cause schizophrenic symptoms, so they are not being used as a therapeutic drug for AD. Memantine does not have those toxicities and does not stimulate acetylcholine release in the cerebral cortex. Although the mechanism of the difference from memantine and MK-801 has not been made clear yet, it seems that memantine is combined and released with the ion channel depending on electric potential in the same way as the magnesium ion. Basic and clinical research will clarify the control mechanism of memantine.
Kato
Takeshi
T
Laboratories of Molecular Recognition and Natural Information Science, Graduate School of Integrated Science, Yokohama City University. tkato@yokohama-cu.ac.jp
D000544:Alzheimer Disease / Q000188:drug therapy*; D001665:Binding Sites; D018849:Controlled Clinical Trials as Topic; D016291:Dizocilpine Maleate / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology / Q000627:therapeutic use*; D005971:Glutamates / Q000378:metabolism; D006801:Humans; D007473:Ion Channels / Q000378:metabolism; D008274:Magnesium / Q000502:physiology; D008559:Memantine / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012720:Severity of Illness Index
D018691:Excitatory Amino Acid Antagonists; D005971:Glutamates; D007473:Ion Channels; D016194:Receptors, N-Methyl-D-Aspartate; D016291:Dizocilpine Maleate; D008274:Magnesium; D008559:Memantine