Competitive, selective, GluA2 (GluR2)-lacking AMPA receptor blocker
Competitive, selective, voltage-dependent open-channel Ca2+ permeable GluA2 (GluR2)-lacking AMPA receptor blocker (IC50 values are 2.6 and 1102 µM at GluA2-lacking and GluA2-containing AMPARs respectively).
IEM-1460 can be utilized as an indicator of the distribution of AMPA receptor subtypes among populations of brain cells.
IEM-1460 can also be used to selectively target GABAergic interneurons, as several subpopulations of these neurons express a significant proportion of GluA2-lacking Ca2+-permeable AMPARs.
Blocks synaptic excitation of fast-spiking interneurons and blocks NMDAR-mediated currents.
Also shows anticonvulsant properties.
N,N,N-Trimethyl-5-[(tricyclo[184.108.40.206,7]dec-1-ylmethyl)amino]-1-pentanaminium bromide hydrobromide
Storing and Using Your Product
room temperature (desiccate)
soluble in water (100mM) or DMSO (100mM)
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References for IEM-1460
The open channel blocking drug, IEM-1460, reveals functionally distinct alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors in rat brain neurons.Samoilova et al (1999) Neuroscience 94(1) : 261-8PubMedID: 10613516
Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460.Buldakova et al (1999) Brain Res 846(1) : 52-8PubMedID: 10536213
Two mechanisms of action of the adamantane derivative IEM-1460 at human AMPA-type glutamate receptors.Schlesinger et al (2005) Br J Pharmacol 145(5) : 656-63PubMedID: 15834439
Selective inhibition of striatal fast-spiking interneurons causes dyskinesias.Gittis et al (2011) J Neurosci 31(44) : 15727-31PubMedID: 22049415