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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.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
16 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 mor. treatment is associated with synaptic increase of GluA4-containing AMPAR in the dorsal horn of the spinal cord. Neuropsychopharmacology 38 1472 PMID: 23403695
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
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
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
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
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
Purkey et al (2018) AKAP150 Palmitoylation Regulates Synaptic Incorporation of Ca2+-Permeable AMPA Receptors to Control LTP. Cell Rep 25 974 PMID: 30355502
Suyama et al (2017) Plasticity of calcium-permeable AMPA glutamate receptors in Pro-opiomelanocortin neurons. Elife 6 PMID: 28762946
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
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
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
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Literature in this Area
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.