AI Article Synopsis

  • Polyvalent cations, which block excitatory responses, were shown to inhibit the binding of a specific radiolabeled compound ([3H]MK-801) to NMDA receptor channels in the brain.
  • The study identified the potency of these cations, ranking Zn2+ as the most effective, followed by La3+ and Cd2+, while Mn2+, Co2+, Ni2+, and Mg2+ were less effective.
  • These results suggest that there are specific sites on NMDA channels where these cations and other antagonists interact, revealing how these cations can influence excitatory neurotransmission and reduce excitotoxicity in the brain.

Article Abstract

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.

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http://dx.doi.org/10.1016/0304-3940(88)90663-5DOI Listing

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