S1RA (E-52862)

S1RA (E-52862) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50 σ1=17 nM, σ2=9300 nM) S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1-dependent manner. S1RA potentiated µ-opioid antinociception in mice in a σ-dependent manner. Also displays neuroprotective effects in a mouse model of ischemic stroke.

Catalog ID: CV-1038

$162.00$570.00

  • Product Details

    • Physical State: Off-white powder
    • Temperature Storage: -20°C
    • Temperature Shipping: Ambient
    • Molecular Mass: 373.9
  • References

    1. Romero, L., et al., (2012) Br. J. Pharmacol., 166 : 2289
    2. Diaz, J.L., et al., (2012) J. Med. Chem., 55 : 8211
    3. Tejada, M.A., et al., (2017) Proc. Natl. Acad. Sci. USA, 114 : 8396
    4. Sanchez-Fernandez, C., et al., (2014) J. Pharmacol. Exp. Ther., 348 : 32
    5. Sanchez-Blazquez, P., et al., (2018) Mol. Neurobiol., 55 : 4940