Therapeutic brain concentration of the NMDA receptor antagonist amantadine

@article{Kornhuber1995TherapeuticBC,
  title={Therapeutic brain concentration of the NMDA receptor antagonist amantadine},
  author={Johannes Kornhuber and G{\"u}nter Quack and Wojciech Danysz and Kurt A. Jellinger and Walter Danielczyk and Wieland Gsell and Peter Franz Riederer},
  journal={Neuropharmacology},
  year={1995},
  volume={34},
  pages={713-721}
}
Amantadine (1-amino-adamantane) is clinically used for the management of Parkinson's disease and drug-induced extrapyramidal symptoms. It has previously been shown that amantadine is a low-affinity uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist with rapid blocking and unblocking channel kinetics (Ki-value at the PCP binding site = 10 microM). The aim of the present studies was to estimate concentrations of amantadine in the central nervous system under therapeutic conditions. In… Expand
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TLDR
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Striatal Kir2 K+ channel inhibition mediates the antidyskinetic effects of amantadine.
TLDR
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