Orphenadrine

Orphenadrine ((±) -Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation[1][2][3].

Product Specifications

CAS Number

[83-98-7]

Product Name Alternative

(±) -Orphenadrine

UNSPSC

12352005

Target

Cholinesterase (ChE) ; Cytochrome P450; iGluR

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/orphenadrine.html

Purity

99.71

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CN(C)CCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2

Molecular Formula

C18H23NO

Molecular Weight

269.38

References & Citations

[1]Kornhuber J, et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102 (3) :237-46.|[2]Pubill D, et al. Orphenadrine prevents 3-nitropropionic acid-induced neurotoxicity in vitro and in vivo. Br J Pharmacol. 2001 Feb;132 (3) :693-702.|[3]Morita R, et al. Liver tumor promoting effect of orphenadrine in rats and its possible mechanism of action including CAR activation and oxidative stress. J Toxicol Sci. 2013;38 (3) :403-13.