Orphenadrine

CAS No:
83-98-7 Category:
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Product Details:

  • CAS No: 83-98-7
  • AHFC code: 12:20.0
  • Synonyms: Mephenamine O-Methyldiphenhydramine Orphenadine Orphenadrin Orphenadrine Citrate Orphenate Orphenedrine
  • ATC Code: M03BC01 N04AB02
  • Chemical Formula: C15H11ClN2O2
  • Molecular Weight: 269.3813
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01173 (APRD00097)
  • SMILES: CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C
  • InChl: QVYRGXJJSLMXQH-UHFFFAOYSA-N
  • PubChem: 4601
  • IUPAC: dimethyl({2-[(2-methylphenyl)(phenyl)methoxy]ethyl})amine

Additional Details

Indication:
Indicated for the treatment of Parkinson's disease.
Pharmacodynamics:
Orphenadrine is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculoskeletal conditions. Orphenadrine is an anticholinergic with a predominantly central effect and only a weak peripheral effect. In addition, it has mild antihistaminic and local anaesthetic properties. Parkinson's syndrome is the consequence of a disturbed balance between cholinergic and dopaminergic neurotransmission in the basal ganglia caused by a decrease in dopamine. Orphenadrine restores the physiological equilibrium and has a favourable effect on the rigidity and tremor of Parkinson's disease and Parkinsonian syndromes. The effect is somewhat less on bradykinesia.
Mode of Action:
Orphenadrine binds and inhibits both histamine H1 receptors and NMDA receptors. It restores the motor disturbances induced by neuroleptics, in particular the hyperkinesia. The dopamine deficiency in the striatum increases the stimulating effects of the cholinergic system. This stimulation is counteracted by the anticholinergic effect of orphenadrine. It may have a relaxing effect on skeletal muscle spasms and it has a mood elevating effect.
Metabolism:
Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.
Toxicity:
Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
General Reference:
Ji D, Sui ZY, Ma YY, Luo F, Cui CL, Han JS: NMDA receptor in nucleus accumbens is implicated in morphine withdrawal in rats. Neurochem Res. 2004 Nov;29(11):2113-20. Pubmed
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