Description
IEM 1460 is an adamantine derivative that blocks both AMPA-
and NMDA-
type glutamate receptor (GluR) channels (IC
50 = 10 μM-0.1 mM). It is selective for Ca
2+-
permeable GluR channels, which lack the GluR2 R subunit, and has been used to identify Ca
2+-
permeable glutamate receptors in the brain.
Biological Activity
Voltage-dependent open-channel blocker of AMPA receptors. Displays selectivity between subtypes, blocking GluR2 subunit-lacking (Ca 2+ -permeable) receptors more potently than GluR2-containing receptors (IC 50 values are 2.6 and 1102 μ M respectively). Also blocks NMDA receptor-mediated currents. Anticonvulsant in vivo .
