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CGS 20625

A Partial Agonist of GABA(A) Receptors
Cat #: C-390
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 309.36
    Purity: >99%
    Effective concentration 1-100 µM.
    Structure
    Chemical name 5,6,7,8,9,10-Hexahydro-2-(4-methoxyphenyl)cyclohepta[b]pyrazolo[3,4-d]pyridin-3(2H)-one.
    Molecular formula C18H19N3O2.
    CAS No.: 111205-55-1.
    PubChem CID 163844
    Activity CGS 20625 acts as a partial agonist at GABA(A) receptors (EC50 = 11.2-23.7 µM)1. It is a potent and selective non-benzodiazepine ligand at the central benzodiazepine receptor (IC50 = 1.3 nM), with anxiolytic and anticonvulsant effects in vivo2.
    References-Activity
    1. Khom, S. et al. (2006) Mol. Pharmacol. 69, 640.
    2. Williams, M. et al. (1989) J. Pharmacol. Exp. Ther. 248, 89.
    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 +4°C.
    Solubility Soluble in DMSO and ethanol. Centrifuge before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs CGS 20625 activates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs CGS 20625 activates GABA(A) receptors expressed in Xenopus oocytes.
      Representative time course of GABA(A) α1/β2 receptor current, activated by 10 µM and 100 µM CGS 20625 (#C-390), as indicated (bars), at a holding potential of -60 mV.
    References - Scientific background
    1. Bennett, D.A. (1987) Physiol. Behav. 41, 241.
    2. Williams, M. et al. (1989) J. Pharmacol. Exp. Ther. 248, 89.
    3. Atack, J.R. (2003) Curr. Drug Targets CNS Neurol. Disord. 2, 213.
    4. Pomara, N. et al. (2015) Prog Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    Scientific background

    CGS 20625 is a synthetic compound that acts as a potent and selective partial agonist of GABA(A) receptors.

    CGS 20625 is a pyrazolopyridine compound that possesses anxiolytic and anticonvulsant characteristics. It binds to a specific recognition site on GABAA receptors containing α1, α2, α3, and α5 subunits1-3.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA actions, a major inhibitory neurotransmitter, throughout the central nervous system where it plays an important role in inhibiting cell excitation. GABA(A) receptors are a major target for antiseizure drugs4.

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

    CGS 20625 (#C-390) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
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