IEM 1460

Catalog #: 1636
16 Citations Datasheet / COA / SDS

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IEM 1460 | CAS No. 121034-89-7 | AMPA Receptor Blockers

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Description: Open-channel blocker of AMPA currents; selective for non-GluA2-containing receptors

Chemical Name: N,N,H,-Trimethyl-5-[(tricyclo[3.3.1.13,7]dec-1-ylmethyl)amino]-1-pentanaminiumbromide hydrobromide

Purity: ≥98%

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Product Details

Citations (16)

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Biological Activity

IEM 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.

Technical Data

M.Wt:

454.33

Formula:

C₁₉H₃₇N₂Br.HBr

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

≥98%

Storage:

Desiccate at RT

CAS No:

121034-89-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

Acquisition of contextual discrimination involves the appearance of a RAS-GRF1/p38 mitogen-activated protein (MAP) kinase-mediated signaling pathway that promotes long term potentiation (LTP).
Jin, Shan-Xue, Arai, Junko, Tian, Xuejun, Kumar-Singh, Rajendra, Feig, Larry A
J Biol Chem, 2013;288(30):21703-13.
Selective inhibition of striatal fast-spiking interneurons causes dyskinesias.
Gittis et al.
J.Neurosci., 2012;31:15727
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.
Br.J.Pharmacol., 2005;145:656

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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.
Elife 2017;6
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.
Front.Cell.Neurosci. 2016;10:50
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.
Neuropsychopharmacology 2013;38:1472
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.
Pain 2011;152:912

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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