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  • 标题:Ca2+ Inhibits the Association of Memantine with N-Methyl-D-aspartate (NMDA) Receptor-Gated Ion Channels
  • 本地全文:下载
  • 作者:Masafumi Fujimoto ; Hirokazu Iida ; Tomoo Homma
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2008
  • 卷号:31
  • 期号:9
  • 页码:1813-1815
  • DOI:10.1248/bpb.31.1813
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:We examined the effect of 1-amino-3,5-dimethyladamantane (memantine) and (+)-5-methyl-10,11-dihydro-5 H -dibenzo[ a , d ]cyclohepten-5,10-imine (MK-801) on the inhibition of [3H]MK-801 binding to crude synaptic membranes of rat forebrains in the absence or presence of Ca2+. Ca2+ decreased the potency of memantine to inhibit [3H]MK-801 binding. The effect of Ca2+ was apparently competitive with memantine and was not annulled by the addition of Mg2+. Ca2+ slightly enhanced [3H]MK-801 binding, but showed no effect on the displacement of [3H]MK-801 binding by MK-801. The Ca2+-sensitive interaction of memantine with N -methyl- D -aspartate (NMDA) receptor-gated ion channels may provide a clue to understanding its voltage-dependent and clinically tolerated character.
  • 关键词:memantine;N-methyl- D -aspartate receptor-gated ion channel;calcium ion;(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801)
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