IEM 1460

Cat. No. 1636

IEM 1460 C19H37N2Br.HBr [121034-89-7]

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

Biological Activity

Voltage-dependent open-channel blocker of AMPA receptors. Selective for GluR2 subunit-lacking (Ca2+-permeable) receptors over GluR2-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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Gittis et al (2012) Selective inhibition of striatal fast-spiking interneurons causes dyskinesias. J.Neurosci. 31 15727. PMID: 22049415.

Schlesinger et al (2005) Two mechanisms of action of the adamantane derivative IEM-1460 at human AMPA-type glutamate receptors. Br.J.Pharmacol. 145 656. PMID: 15834439.

Buldakova et al (1999) Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460. Brain Res. 846 52. PMID: 10536213.

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Citations are publications that use Tocris products. Selected citations for IEM 1460 include:

Kopach et al (2016) Inhibition of spinal Ca(2+)-permeable AMPA receptors with dicationic compounds alleviates persistent inflammatory pain without adverse effects. Front.Cell.Neurosci. 10 50. PMID: 26973464.

Park et al (2016) Calcium-Permeable AMPA Receptors Mediate the Induction of the Protein Kinase A-Dependent Component of Long-Term Potentiation in the Hippocampus. J Neurosci 36 622. PMID: 26758849.

Liu et al (2015) Long-term upregulation of cortical glutamatergic AMPA receptors in a mouse model of chronic visceral pain. Mol Brain 8 76. PMID: 26585043.

Tang et al (2015) Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex. J Pharmacol Exp Ther 5 14099. PMID: 26370265.

Höft et al (2014) Heterogeneity in expression of functional ionotropic glutamate and GABA receptors in astrocytes across brain regions: insights from the thalamus. Philos Trans R Soc Lond B Biol Sci 369 20130602. PMID: 25225096.

Cabañero et al (2013) Pain after discontinuation of morphine treatment is associated with synaptic increase of GluA4-containing AMPAR in the dorsal horn of the spinal cord. Neuropsychopharmacology 38 1472. PMID: 23403695.

Chen et al (2013) Nerve injury increases GluA2-lacking AMPA receptor prevalence in spinal cords: functional significance and signaling mechanisms. PLoS Negl Trop Dis 347 765. PMID: 24030012.

Colgan et al (2012) Action potential-independent and pharmacologically unique vesicular serotonin release from dendrites. J Neurosci 32 15737. PMID: 23136413.

Fortin et al (2012) 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. J Neurosci 32 8127. PMID: 22699894.

Case et al (2011) Functional refinement in the projection from ventral cochlear nucleus to lateral superior olive precedes hearing onset in rat. PLoS One 6 e20756. PMID: 21694776.

Kopach et al (2011) Inflammation alters trafficking of extrasynaptic AMPA receptors in tonically firing lamina II neurons of the rat spinal dorsal horn. Pain 152 912. PMID: 21282008.

Hildebrand et al (2009) Functional coupling between mGluR1 and Cav3.1 T-type calcium channels contributes to parallel fiber-induced fast calcium signaling within Purkinje cell dendritic spines. J Neurosci 29 9668. PMID: 19657020.

Santos et al (2009) Transmission efficacy and plasticity in glutamatergic synapses formed by excitatory interneurons of the substantia gelatinosa in the rat spinal cord. PLoS One 4 e8047. PMID: 19956641.

Guire et al (2008) Recruitment of calcium-permeable AMPA receptors during synaptic potentiation is regulated by CaM-kinase I. Sci Rep 28 6000. PMID: 18524905.

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Keywords: IEM 1460, supplier, Open-channel, blockers, AMPA, currents, selective, non-GluR2-containing, receptors, NMDA, blocks, Glutamate, Receptors, iGluR, Ionotropic, N-Methyl-D-Aspartate, IEM1460, neuron, neurones, medium, spiny, neurons, fast, spiking, interneurons, MSNs, FSIs, Tocris Bioscience, AMPA Receptor Blocker products

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