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Tracazolate hydrochloride

ICI 136753
A Modulator of GABA(A) Receptors
Cat #: T-230
Alternative Name ICI 136753
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 340.85
    Purity: >99%
    Effective concentration 10-100 µM.
    Structure
    Chemical name Ethyl-4-(butylamino)-1-ethyl-6-methylpyrazolo[3,4-b]pyridine-5-carboxylate;hydrochloride.
    Molecular formula C16H25ClN4O2.
    CAS No.: 41094-88-6.
    PubChem CID 24871267
    Activity Tracazolate is an allosteric modulator of GABA(A) receptors, that was shown to potentiate (EC50 = 1.1-16.7 µM) or inhibit (IC50 = 1.2-4.0 µM) GABA-evoked currents in a subunit combination dependent manner1.
    References-Activity
    1. Thompson, S.A. et al. (2002) Mol. Pharmacol. 61, 861.
    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 desiccated at -20°C. Protect from light.
    Solubility Soluble in 1eq. HCl and in DMSO. Centrifuge all product preparations before use (10000 x g, 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Tracazolate hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Tracazolate hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.
      Time course of GABA(A) α1/β2 currents, reversibly activated in a concentration dependent manner by 10 µM, 35 µM and 100 µM Tracazolate hydrochloride (#T-230) while membrane potential was held at -60 mV.
    References - Scientific background
    1. Thompson, S.A. et al. (2002) Mol. Pharmacol. 61, 861.
    2. Zheleznova, N. et al. (2008) Br. J. Pharmacol. 153, 1062.
    3. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    4. Iqbal, F. et al. (2011) Bioorg. Med. Chem. Lett. 21, 4252.
    Scientific background

    Tracazolate hydrochloride, a pyrazolopyridine, is a non-sedative anxiolytic compound that acts as an allosteric modulator of GABA(A) receptors. Tracazolate was shown to potentiate the GABA(A) receptor with an EC50 value of 1.1 µM and inhibit with an IC50 value of 1.2 µM1.

    In addition to its anxiolytic activity, tracazolate possesses anticonvulsant activity that was shown in behavioral studies. Tracazolate seems to cause less adverse interactions in combination with barbiturates and alcohol and demonstrates a wider separation between sedative and therapeutic doses than the benzodiazepines1,2.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system. They also play an important role in inhibiting cell excitation in the central nervous system, and are considered to be a major target of antiseizure drugs3,4.

    Target GABA(A) receptors
    Last update: 23/08/2020

    Tracazolate hydrochloride (#T-230) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information