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A Positive Allosteric Modulator of GABA(A) Receptors

Cat #: S-215
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 354.4
    Purity: >97%
    Effective concentration 1-100 µM.
    Chemical name (6-fluoro-2-methyl-3,4-dihydro-2H-quinolin-1-yl)-(2-pyrazin-2-yl-1,3-thiazol-4-yl)methanone.
    Molecular formula C18H15FN4OS.
    CAS No.: 1234977-97-9
    PubChem CID 49713517
    Activity SJM-3 is a novel positive allosteric modulator of GABA(A) receptors at the benzodiazepine modulatory site (pKi = 6.7), strongly potentiating GABA currents at 30 µM via the binding site for diazepam in the transmembrane domain, while acting as an antagonist at the α+/γ− site1.
    1. Middendorp, S.J. et al. (2015) Neuropharmacology 95, 459.
    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 handling (10000 x g, 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs SJM-3 potentiates GABA(A) receptors expressed in Xenopus oocytes.
      Alomone Labs SJM-3 potentiates 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). Currents are significantly enhanced by co-application of 50 µM SJM-3 (#S-215), as indicated (bar), at a holding potential of -60 mV.
    References - Scientific background
    1. Middendorp, S.J. et al. (2015) Neuropharmacology 95, 459.
    2. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    Scientific background

    SJM-3 is a positive allosteric modulator of γ-aminobutyric acid type A (GABA(A)) receptors. It potentiates GABA(A) receptor currents by binding at the diazepam binding site in the transmembrane domain. SJM-3 was also shown to act as an antagonist at the α+/γ− site of the receptor1.

    GABA(A) receptors belong to the cys-loop pentameric ligand-gated ion channel family. These receptors are major inhibitory neurotransmitter receptors in the brain and in the mammalian central nervous system and are responsible for mediating GABA action. They are composed of five homologous subunits that are arranged around a central chloride-selective pore. GABA(A) receptors are important targets for many clinical drugs1,2.

    Target GABA(A) receptors
    Last update: 06/11/2022

    SJM-3 (#S-215) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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