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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 yes
  • Bioassay Tested
    • Source Synthetic
    MW: 415.39
    Purity: >98% (HPLC)
    Effective concentration 0.1-10 µM.
    Structure
    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.
    References-Activity
    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.
    Our bioassay
    • Alomone Labs GABA(A)-Compound 1b inhibits GABA(A) receptors expressed in Xenopus oocytes.
      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.
    Scientific background

    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
    Lyophilized Powder
    Last update: 02/01/2022

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

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    For research purposes only, not for human use
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