A muscarinic acetylcholine receptor antagonist
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Orphenadrine (hydrochloride)

Item No. 26391

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,N-dimethyl-2-[(2-methylphenyl)phenylmethoxy]-ethanamine, monohydrochloride
CAS Number
341-69-5
Synonyms
  • NSC 82357
Molecular Formula
C18H23NO • HCl
Formula Weight
305.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlEthanol: 10 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
CN(C)CCOC(C1=CC=CC=C1C)C2=CC=CC=C2.Cl
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
InChi Key
UQZKYYIKWZOKKD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $54

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    25 mg

    $127

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    50 mg

    $238

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    Product Description

    Orphenadrine is a muscarinic acetylcholine receptor (mAChR) antagonist (Kds = 48, 213, 120, 170, and 129 nM for M1-M5 receptors, respectively).1 Orphenadrine (2-5 mg/kg, i.v.) decreases muscle activity induced by the mAChR agonist oxotremorine in rabbits.2 It is also an NMDA receptor antagonist with a Ki value of 6 µM in a radioligand binding assay in human postmortem frontal cortex and an IC50 value of 16.2 µM for inhibiting steady state currents in cultured superior colliculus neurons.3 Formulations containing orphenadrine have been used in the treatment of acute painful musculoskeletal conditions, including muscle spasms.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stanton, T., Bolden-Watson, C., Cusack, B., et al. Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics. Biochem. Pharmacol. 45(11), 2352-2354 (1993).

    2. Ban, T., and Hojo, M. A comparative study of the effects of anti-parkinson drugs on the oxotremorine-induced EEG and muscular activities. Psychopharmacologia 19(1), 1-15 (1971).

    3. Kornhuber, J., Parsons, C.G., Hartmann, S., et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: Binding and patch clamp studies. J. Neural Transm. Gen. Sect. 102(3), 237-246 (1995).