IEM 1460

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Cat.No. 1636 - IEM 1460 | C19H37N2Br.HBr | CAS No. 121034-89-7
Description: Open-channel blocker of AMPA currents; selective for non-GluR2-containing receptors
Chemical Name: N,N,H,-Trimethyl-5-[(tricyclo[3.3.1.13,7]dec-1-ylmethyl)amino]-1-pentanaminiumbromide hydrobromide
Purity: ≥98% (HPLC)
Datasheet
Citations (14)
Literature

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.

Compound Libraries

IEM 1460 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 454.33
Formula C19H37N2Br.HBr
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 121034-89-7
PubChem ID 6604954
InChI Key CQTDZUSQSTUZDA-UHFFFAOYSA-M
Smiles [Br-].Br.C[N+](C)(C)CCCCCNCC12CC3CC(C1)CC(C2)C3

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.43 100
water 45.43 100
phosphate buffered saline 45.43 100

Preparing Stock Solutions

The following data is based on the product molecular weight 454.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.2 mL 11.01 mL 22.01 mL
5 mM 0.44 mL 2.2 mL 4.4 mL
10 mM 0.22 mL 1.1 mL 2.2 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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


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View all AMPA Receptor Blockers

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, AMPA, Receptors, NMDA, Receptors, AMPA, Receptors, Tocris Bioscience

14 Citations for IEM 1460

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

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

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

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

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

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

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

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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