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A Positive Allosteric Modulator of AMPA Receptors

Cat #: C-205
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 389.9
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Chemical name 6-Chloro-3,4-dihydro-3-(2-norbornen-5-yl)-2H-1,2-4-benzothiadiazine-7-sulfonamide 1,1-dioxide.
    Molecular formula C14H16ClN3O4S2.
    CAS No.: 2259-96-3
    Activity Cyclothiazide is a selective AMPA receptor agonist (allosteric potentiator)1.
    1. Johansen, T.H. et al. (1995) Mol. Pharmacol. 48, 946.
    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 Cyclothiazide potentiates GluA1 channels expressed in Xenopus oocytes.
      Alomone Labs Cyclothiazide potentiates GluA1 channels expressed in Xenopus oocytes.
      Time course of current reversible potentiation by 1, 10 and 100 μM Cyclothiazide (#C-205) of glutamate-elicited currents (100 μM, holding potential -80 mV).
    References - Scientific background
    1. Fucile, S. et al. (2006) Proc. Natl. Acad. Sci. U.S.A. 103, 2943.
    Scientific background Cyclothiazide (CTZ) is one of the most potent benzothiadiazides, a class of positive allosteric modulators of non-NMDA-type glutamate receptors, that inhibit receptor desensitization with a marked selectivity for the flip splice variants of AMPA receptors. Specifically, CTZ is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. By using patch-clamp techniques, the effects of CTZ were studied in HEK 293 cells stably transfected with the rat flip GluR1 subunit. The AMPA currents were greatly potentiated by CTZ in a dose-dependent manner. For instance, pretreatment of the cells with 100 μM CTZ increased the peak AMPA current 90-fold (EC50 = 28 μM), the current at the end of AMPA application 636-fold (EC50 = 46 μM), and the current integrals 730-fold (EC50 = 41 μM)1.
    Target AMPA receptors
    Last update: 06/11/2022

    Cyclothiazide (#C-205) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    1. Zebrafish brain slices (mEPSC recordings).
      Nakajo, H. et al. (2020) Cell Rep. 31, 107790.


    Scientific Background

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