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 | |||
| phosphate buffered saline | 45.43 | 100 | |
| DMSO | 45.43 | 100 | |
| water | 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
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
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
