GABA(A)-Compound 1b

8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one
A Novel Antagonist of GABA(A) Receptors
    Cat #: CMG-004
    Alternative Name 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 415.39
    Purity: >98% (HPLC)
    Effective concentration 0.1-10 µM.
      • GABA(A)-Compound 1b
    Chemical name 8-Methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one.
    Molecular formula C20H12F3N3O2S.
    Activity A novel antagonist of α5 containing GABA(A) receptors, displaying significant selectivity for α5 (IC50 = 201 nM, Imax = 92%) over α1, α2, α3 and α4 containing receptors, on which it produces only partial maximum inhibition (Imax = 54, 0, 39 and 35%, respectively) at higher concentrations (IC50 = 0.48, >10, 0.48 and 0.91 µM, respectively)1.
      • Ling, I. et al. (2015) Eur. J. Pharmacol. 764, 497.
    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 Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
    Storage of solutions Up to three months at -20°C.
      • GABA(A)-Compound 1b
        Alomone Labs GABA(A)-Compound 1b inhibits GABA(A) receptors expressed in Xenopus oocytes.
        Representative time course of GABA(A) α1/β2 current, activated by a continuous application (top dotted line) of 0.1 µM γ-Aminobutyric acid (#G-110), and partially inhibited by 2 µM GABA(A)-Compound 1b (#CMG-004), as indicated (bar), at a holding potential of -60 mV.
    References - Scientific background
    • 1. Ling, I. et al. (2015) Eur. J. Pharmacol. 764, 497.
    • 2. Williams, M. et al. (1989) J. Pharmacol. Exp. Ther. 248, 89.
      • GABA(A)-Compound 1b (8-methyl-5-[4-(trifluoromethyl)-1-benzothiophen-2-yl]-1,9-dihydro-2H-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one) is a potent and selective antagonist of α5 containing GABA(A) receptors, displaying an IC50 value of 201 nM. On α1-4 containing receptors, the antagonist demonstrates only partial maximum inhibition1.

        GABA(A)-Compound 1b is characterized as a 2,3-benzodiazepine with substantial blood-brain barrier permeability. In vivo studies reveal that 1b is devoid of sedative effects, is pro-convulsive, and enhances the performance of rats in the object recognition test.

        GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter throughout the central nervous system (CNS), thus play an important role in inhibiting cell excitation in the CNS.

        GABA(A) receptors are considered a major target of antiseizure drugs2.

    Target GABA(A) receptors
    Last update: 23/10/2019

    GABA(A)-Compound 1b (#CMG-004) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use