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Orphenadrine

Catalog No. T68599 CAS 83-98-7

Synonyms: Orphenadrine (free base)

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

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Orphenadrine, CAS 83-98-7

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5 mg	In stock	$ 52.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 110.00
50 mg	In stock	$ 158.00
100 mg	In stock	$ 236.00

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Purity: 99.38%

Purity: 99.26%

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Description	Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.
In vitro	Orphenadrine decreased CYP2B6 marker activity up to 45-57% in human liver microsomes and up to 80-97% in cell microsomes containing cDNA-expressed CYP2B6. Orphenadrine strongly decreased CYP2D6 marker activity by 80-90%. Orphenadrine also partially decreased the CYP1A2, CYP2A6, CYP3A4, and CYP2C19 marker activities.[4]
In vivo	Orphenadrine (75 mg/kg/day; i.p.; for 3 days) was associated with a 2-fold induction of total hepatic P-450, a 5- and 2.4-fold induction of androstenedione 16 beta- and 6 beta-hydroxylase activity, respectively, and formation of an orphenadrine-P-450 MI complex. Western blots of orphenadrine-induced microsomes revealed a 20-fold increase in P-450 PB-B/D-immunoreactive protein.[2]

Synonyms	Orphenadrine (free base)
Molecular Weight	269.38
Formula	C18H23NO
CAS No.	83-98-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (185.61 mM)

References and Literature

1. Roos PH, et al. Metabolite complex formation of orphenadrine with cytochrome P450. Involvement of CYP2C11 and CYP3A isozymes. Biochem Pharmacol. 1996;52(1):73-84. 2. Reidy GF, et al. Inhibition of oxidative drug metabolism by orphenadrine: in vitro and in vivo evidence for isozyme-specific complexation of cytochrome P-450 and inhibition kinetics. Mol Pharmacol. 1989;35(5):736-743. 3. Chen YW, et al. Intrathecal orphenadrine elicits spinal block in the rat. Eur J Pharmacol. 2014;742:125-130. 4. Guo Z, et al. Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Drug Metab Dispos. 1997;25(3):390-393. 5. Sureda FX, et al. In vitro and in vivo protective effect of orphenadrine on glutamate neurotoxicity. Neuropharmacology. 1999;38(5):671-677.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library

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Keywords

Orphenadrine 83-98-7 Membrane transporter/Ion channel Neuroscience NMDAR AChR Sodium Channel Orphenadrine (free base) inhibitor inhibit

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