IEM 1460
Biological Activity
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.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 45.43 | 100 | |
| DMSO | 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 the degree 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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References
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for IEM 1460, please let us know.
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Keywords: IEM 1460, 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, GluA2, 1636, Tocris Bioscience
14 Citations for IEM 1460
Citations are publications that use Tocris products. Selected citations for IEM 1460 include:
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
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
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
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
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
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
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
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
Colgan et al (2012) Action potential-independent and pharmacologically unique vesicular serotonin release from dendrites. J Neurosci 32 15737 PMID: 23136413
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
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
Do you know of a great paper that uses IEM 1460 from Tocris? Please let us know.
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