Chemical Name: N,N,H,-Trimethyl-5-[(tricyclo[188.8.131.52,7]dec-1-ylmethyl)amino]-1-pentanaminiumbromide hydrobromide
Biological ActivityIEM 1460 is a voltage-dependent open-channel blocker of AMPA receptors. Selective for GluR2 subunit-lacking (Ca2+-permeable) receptors over GluA2-containing receptors (IC50 values are 2.6 and 1102 μM, respectively). Selectively blocks fast spiking interneuron but not medium spiny projection neuron in mouse striatum. Also blocks NMDA receptor-mediated currents. Anticonvulsant in vivo.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Selective inhibition of striatal fast-spiking interneurons causes dyskinesias.
Gittis et al.
Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460.
Buldakova et al.
Brain Res., 1999;846:52
Two mechanisms of action of the adamantane derivative IEM-1460 at human AMPA-type glutamate receptors.
Schlesinger et al.
Citations for IEM 1460
The citations listed below are publications that use Tocris products. Selected citations for IEM 1460 include:
16 Citations: Showing 1 - 10
AKAP150 Palmitoylation Regulates Synaptic Incorporation of Ca2+-Permeable AMPA Receptors to Control LTP.
Authors: Purkey Et al.
Cell Rep 2018;25:974
Plasticity of calcium-permeable AMPA glutamate receptors in Pro-opiomelanocortin neurons.
Authors: Suyama Et al.
Calcium-Permeable AMPA Receptors Mediate the Induction of the Protein Kinase A-Dependent Component of Long-Term Potentiation in the Hippocampus.
Authors: Park Et al.
J Neurosci 2016;36:622
Inhibition of spinal Ca(2+)-permeable AMPA receptors with dicationic compounds alleviates persistent inflammatory pain without adverse effects.
Authors: Kopach Et al.
Long-term upregulation of cortical glutamatergic AMPA receptors in a mouse model of chronic visceral pain.
Authors: Liu Et al.
Mol Brain 2015;8:76
Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex.
Authors: Tang Et al.
J Pharmacol Exp Ther 2015;5:14099
Heterogeneity in expression of functional ionotropic glutamate and GABA receptors in astrocytes across brain regions: insights from the thalamus.
Authors: Höft Et al.
Philos Trans R Soc Lond B Biol Sci 2014;369:20130602
Pain after discontinuation of mor. treatment is associated with synaptic increase of GluA4-containing AMPAR in the dorsal horn of the spinal cord.
Authors: Cabañero Et al.
Nerve injury increases GluA2-lacking AMPA receptor prevalence in spinal cords: functional significance and signaling mechanisms.
Authors: Chen Et al.
PLoS Negl Trop Dis 2013;347:765
Brain-derived neurotrophic factor activation of CaM-kinase kinase via transient receptor potential canonical channels induces the translation and synaptic incorporation of GluA1-containing calcium-permeable AMPA receptors.
Authors: Fortin Et al.
J Neurosci 2012;32:8127
Action potential-independent and pharmacologically unique vesicular serotonin release from dendrites.
Authors: Colgan Et al.
J Neurosci 2012;32:15737
Functional refinement in the projection from ventral cochlear nucleus to lateral superior olive precedes hearing onset in rat.
Authors: Case Et al.
PLoS One 2011;6:e20756
Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn.
Authors: Kopach Et al.
Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord.
Authors: Santos Et al.
PLoS One 2009;4:e8047
Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines.
Authors: Hildebrand Et al.
J Neurosci 2009;29:9668
Recruitment of calcium-permeable AMPA receptors during synaptic potentiation is regulated by CaM-kinase I.
Authors: Guire Et al.
Sci Rep 2008;28:6000
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