Competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3
= 120 nM) and [3
= 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC50
values range from 2.5 to 11 μ
M). Inhibits currents induced by AMPA, kainate and NMDA with IC50
values of 21 nM, 27 nM, and > 1 μ
M respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo
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Novel α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration.
Elger et al.
X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor.
ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman
Turski et al.
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