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Isoguvacine hydrochloride

An Agonist of GABA(A) Receptors

Cat #: I-185
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 163.6
    Purity: >99%
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name 1,2,3,6-tetrahydropyridine-4-carboxylic acid;hydrochloride.
    Molecular formula C6H10ClNO2.
    CAS No.: 68547-97-7
    PubChem CID 155107
    Activity Isoguvacine hydrochloride is a specific agonist of the GABA(A) receptors, with EC50 of 3.7–17.3 µM, depending on subunit composition1.
    References-Activity
    1. Stórustovu, S.I. and Ebert, B. (2006) J. Pharmacol. Exp. Ther. 316, 1351.‏
    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 Up to 100 mM in water. 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 Isoguvacine hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs Isoguvacine hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.
      Time course of GABA(A) α1/β2 currents activation by 0.1 µM and 1 µM Isoguvacine hydrochloride (#I-185) at a holding potential of -60 mV.
    References - Scientific background
    1. Stórustovu, S.I. and Ebert, B. (2006) J. Pharmacol. Exp. Ther. 316, 1351.‏
    2. White, W.F. and Snodgrass, S.R. (1983) J. Neurochem. 40, 1701.
    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

    Isoguvacine hydrochloride is a specific and potent agonist of GABA(A) receptors with an EC50 value of 3.7–17.3 µM, depending on the subunit composition1. It is a semirigid analogue of trans-4-aminocrotonic acid with limited conformational flexibility and is less potent than GABA1,2.

    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, and play an important role in inhibiting cell excitation in the central nervous system. GABA(A) receptors are considered to be a major target of antiseizure drugs3,4.

    Target GABA(A) receptors
    Lyophilized Powder
    Last update: 25/07/2021

    Isoguvacine hydrochloride (#I-185) is a highly pure, synthetic, and biologically active compound.

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

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