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Opiranserin

Chemical Structure : Opiranserin

CAS No.: 1441000-45-8

Opiranserin (VVZ-149;VVZ-000149)

Catalog No.: PC-60526Not For Human Use, Lab Use Only.

Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM).

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    Biological Activity

    Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM); demonstrates analgesic efficacy for postoperative pain.

    Pain

    Phase 2 Clinical

    Physicochemical Properties

    M.Wt 394.512
    Formula C21H34N2O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    Benzamide, 4-butoxy-N-[[4-(dimethylamino)tetrahydro-2H-pyran-4-yl]methyl]-3,5-dimethoxy-

    References

    1. Nedeljkovic SS, et al. BMJ Open. 2017 Feb 17;7(2):e011035.

    2. Oh J, et al. J Clin Pharmacol. 2018 Jan;58(1):64-73.

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