Ca2+ inhibits the association of memantine with N-methyl-D-aspartate (NMDA) receptor-gated ion channels

被引：3

作者：

Fujimoto, Masafumi ^{[1
]}

Iida, Hirokazu ^{[2
]}

Homma, Tomoo ^{[3
]}

Kimura, Ikuo ^{[1
]}

Mori, Masahiro ^{[1
]}

Hamana, Hiroshi ^{[2
]}

机构：

[1] Chiba Inst Sci, Fac Pharmaceut Sci, Lab Appl Pharmacol, Chiba 2880025, Japan

[2] Chiba Inst Sci, Fac Pharmaceut Sci, Organ Chem Lab, Chiba 2880025, Japan

[3] Chiba Inst Sci, Fac Risk & Crisis Management, Dept Environm Syst Sci, Chiba 2880025, Japan

来源：

BIOLOGICAL & PHARMACEUTICAL BULLETIN | 2008年 / 31卷 / 09期

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);

D O I：

10.1248/bpb.31.1813

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

We examined the effect of 1-amino-3,5-dimethyladamantane (memantine) and (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801) on the inhibition of [H-3]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 [H-3]MK-801 binding. The effect of Ca2+ was apparently competitive with memantine and was not annulled by the addition of Mg2+. Ca2+ slightly enhanced [H-3]MK-801 binding, but showed no effect on the displacement of [H-3]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.

引用

页码：1813 / 1815

页数：3

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