SJM-3

A Positive Allosteric Modulator of GABA(A) Receptors
  • New
Cat #: S-215
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
  • Promotion
  • Lyophilized Powder
  • Bioassay Tested
  • Shipped at Room Temp.
  • Source: Synthetic
    MW: 354.40 Da.
    Purity >97%.
    Effective concentration 1-100 µM.
    Structure
    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 number 1234977-97-9.
    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.
    Storage before reconstitution -20°C.
    Reconstitution Soluble in DMSO. Centrifuge before handling (10000 x g, 5 min).
    Storage after reconstitution -20°C.
    Our bioassay
    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
    1. Middendorp, S.J. et al. (2015) Neuropharmacology 95, 459.
    2. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry 56, 35.
    Target: GABA(A) receptors

    Promotion

    Use code: new-yl30-18
    Valid until January 31st, 2018.

    New website special

    Last update: 25/12/2017

    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.

    Alomone Labs is pleased to offer SJM-3 (#S-215).

    For research purposes only, not for human use