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A Positive Allosteric Modulator of AMPA Receptors

Cat #: I-140
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 232.7
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 10-500 µM.
    Chemical name 7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide.
    Molecular formula C8H9ClN2O2S.
    CAS No.: 22503-72-6
    Activity IDRA 21 is a selective AMPA receptor agonist1.
    1. Arai, A. et al. (1996) Neuroreport 7, 2211.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs IDRA 21 potentiates GluA1 channels expressed in Xenopus oocytes.
      Alomone Labs IDRA 21 potentiates GluA1 channels expressed in Xenopus oocytes.
      Time course of current reversible potentiation by 100 and 500μM IDRA 21 (#I-140) of glutamate-elicited currents (100 μM, holding potential -80 mV).
    References - Scientific background
    1. Buccafusco, J.J. et al. (2004) Neuropharmacology 46, 10.
    Scientific background IDRA 21 is a well characterized benzothiadiazine positive allosteric modulator of glutamate AMPA receptors. IDRA 21 produced a concentration-dependent inhibition of glutamate-induced inactivation of membrane currents in recombinant HEK 293 (human embryonic kidney) cells stably transfected with human GluR1/2 flip receptors. IDRA 21 doubled the charge transfer at a concentration of 70 μM, suggesting that this compound can facilitate excitatory neurotransmission via GluR 1/2 receptors. The drug originally considered in the nootropic class of agents (which have had limited success as cognitive-enhancing agents clinically) has been shown to inhibit the rate of desensitization of the AMPA receptor during prolonged exposure to competitive agonists. Thus, the drug acts to strengthen glutamatergic synapses and requires the release of endogenous glutamate for its pharmacological actions. This property of IDRA 21 supports its ability to enhance long-term potentiation (LTP), particularly within the hippocampus1.
    Target AMPA receptors
    Last update: 13/10/2022

    IDRA 21 (#I-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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