Cation interactions with putative NMDA receptor-gated channels labeled by [3H]MK-801 in rat cerebral cortex.
Polyvalent cations that block excitatory responses to N-methyl-D-aspartate inhibited the binding of [3H]MK-801 to putative N-methyl-D-aspartate receptor-gated channels in brain membranes. The order of potency was Zn2+ greater than La3+ = Cd2+ greater than Mn2+ greater than Co2+ greater than Ni2+ = Mg2+. These findings support the existence of interacting sites on the N-methyl-D-aspartate channel for ionic and organic antagonists, and provide a molecular mechanism for the modulation of excitatory neurotransmission and excitotoxicity by endogenous polyvalent cations.
Greenberg
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DA
Department of Neurology, University of California, San Francisco General Hospital 94110.
Marks
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D000818:Animals; D001667:Binding, Competitive; D002413:Cations, Divalent / Q000378:metabolism*; D003986:Dibenzocycloheptenes / Q000378:metabolism*; D016291:Dizocilpine Maleate; D007811:Lanthanum / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology
D002413:Cations, Divalent; D003986:Dibenzocycloheptenes; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; D007811:Lanthanum; D016291:Dizocilpine Maleate