Voltage- and use-dependent open-channel antagonist of AMPA receptors. Selective between subtypes; blocks GluR2 subunit-lacking receptors more potently than GluR2-containing receptors (KD
for GluR2-containing AMPAR is 210 times higher at -80 mV). More potent than IEM 1460
(Cat. No. 1636) and IEM 1754
(Cat. No. 4199) due to a slower unblocking rate. Alleviates inflammatory pain in a rat model of peripheral inflammation.
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Voltage-dependent block of native AMPA receptor channels by dicationic compounds.
Tikhonov et al.
Inhibition of spinal Ca2+-permeable AMPA receptors with dicationic compounds alleviates persistent inflammatory pain without adverse effects.
Kopach et al.
Front.Cell Neurosci., 2016;10