Product overview

  • Name
    IEM-1460
  • Short description
    Competitive, selective, GluA2 (GluR2)-lacking AMPA receptor blocker
  • Biological description

    Competitive, selective, voltage-dependent open-channel Ca2+ permeable GluA2 (GluR2)-lacking AMPA receptor blocker (IC50 values are 2.6 and 1102 µM at GluA2-lacking and GluA2-containing AMPARs respectively).


    IEM-1460 can be utilized as an indicator of the distribution of AMPA receptor subtypes among populations of brain cells.

    IEM-1460 can also be used to selectively target GABAergic interneurons, as several subpopulations of these neurons express a significant proportion of GluA2-lacking Ca2+-permeable AMPARs.


    Blocks synaptic excitation of fast-spiking interneurons and blocks NMDAR-mediated currents.

    Also shows anticonvulsant properties.

  • Biological action
    Blocker
  • Our products in action

Properties

  • Chemical name
    N,N,N-Trimethyl-5-[(tricyclo[3.3.1.13,7]dec-1-ylmethyl)amino]-1-pentanaminium bromide hydrobromide
  • Molecular Weight
    454.33
  • Chemical structure
    IEM-1460  [121034-89-7]
  • Molecular Formula
    C19H37BrN2.HBr
  • CAS Number
    121034-89-7
  • SMILES
    [Br-].Br.C[N+](C)(C)CCCCCNCC13CC2CC(CC(C1)C2)C3

Storing and Using Your Product

  • Storage instructions
    room temperature (desiccate)
  • Solubility overview
    soluble in water (100mM) or DMSO (100mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for IEM-1460

  • The open channel blocking drug, IEM-1460, reveals functionally distinct alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors in rat brain neurons.

    Samoilova et al (1999) Neuroscience 94(1) : 261-8
    PubMedID: 10613516
  • Characterization of AMPA receptor populations in rat brain cells by the use of subunit-specific open channel blocking drug, IEM-1460.

    Buldakova et al (1999) Brain Res 846(1) : 52-8
    PubMedID: 10536213
  • Two mechanisms of action of the adamantane derivative IEM-1460 at human AMPA-type glutamate receptors.

    Schlesinger et al (2005) Br J Pharmacol 145(5) : 656-63
    PubMedID: 15834439
  • Selective inhibition of striatal fast-spiking interneurons causes dyskinesias.

    Gittis et al (2011) J Neurosci 31(44) : 15727-31
    PubMedID: 22049415