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    Orphenadrine Citrate
    Orphenadrine Citrate

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1190
    CAS #: 4682-36-4Purity ≥98%

    Description: Orphenadrine Citrate (BS-5930; BS5930; BS 5930; Disipal), the citrate salt of Orphenadrine, is an uncompetitive NMDA receptor antagonist and a potent skeletal muscle relaxant with antispastic and analgesic activities. Orphenadrine has been used to treat drug-induced parkinsonism and to relieve pain from muscle spasm, also used as an antispastic and analgesic drug.  

    References: J Neural Transm Gen Sect. 1995;102(3):237-46; Eur J Clin Pharmacol. 1982;21(4):343-50.

    Related CAS #: 341-69-5 (HCl)   83-98-7 (free)  4682-36-4 (citrate)

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    Molecular Weight (MW)461.5 
    FormulaC18H23NO.C6H8O7 
    CAS No.4682-36-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 92 mg/mL (199.3 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: N,N-dimethyl-2-(phenyl(o-tolyl)methoxy)ethan-1-amine hydrochloride

    InChi Key: UQZKYYIKWZOKKD-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H23NO.ClH/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16;/h4-12,18H,13-14H2,1-3H3;1H

    SMILES Code: CC1=CC=CC=C1C(OCCN(C)C)C2=CC=CC=C2.[H]Cl           

    Synonyms

    BS 5930, BS5930, Orphenadrine Hydrochloride, BS-5930, Disipal, Orphenadrine HCl


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    In Vitro

    In vitro activity: Orphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug. Orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a Ki-value of 6.0 +/- 0.7 microM. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration- and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 +/- 1.6 microM (n = 6). Orphenadrine exhibited relatively fast, concentration-dependent open channel blocking kinetics (Kon 0.013 +/- 0.002 10(6) M-1S-1) whereas the offset rate was concentration-independent (Koff 0.230 +/- 0.004 S-1). Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05+/-0.20 microM). It can be concluded that orphenadrine, at low micromolar concentrations, interacts with the noradrenaline reuptake system inhibiting its functionality and thus potentiating the effect of noradrenaline.

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    References

    J Neural Transm Gen Sect. 1995;102(3):237-46; Eur J Clin Pharmacol. 1982;21(4):343-50.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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