General
Preferred name
ORPHENADRINE
Synonyms
ORPHENADRINE CITRATE ()
Orphenadrine hydrochloride ()
ORPHENADRINE (CHLORIDE) ()
Mebedrol ()
Mephenamin ()
Flexon ()
Flexoject ()
Banflex ()
Orphenadrine (free base) ()
Norflex4682-36-4 ()
Orphenadrine (citrate) ()
(±)-Orphenadrine ()
Norflex ()
NSC-757238 ()
Orphenadrine dihydrogen citrate ()
Orphenadrine citrate component of invagesic forte ()
Orphenadrine citrate component of orphengesic ()
Orphenadrine citrate component of orphengesic forte ()
Orphenadrine citrate component of norgesic ()
Orphenadrine citrate component of invagesic ()
(¡À)-Orphenadrine ()
Orphengesic ()
Orfenadrina ()
Mialgin ()
Invagesic ()
Mefenamine ()
Orphenadrin ()
Norgesic ()
Disipal ()
Orphenadrine HCl ()
Orphenadrine (chloride) ()
NSC-82357 ()
Orphenadrine (hydrochloride) ()
P&D ID
PD009762
CAS
4682-36-4
83-98-7
4596-23-0
4724-58-7
341-69-5
Tags
available
drug
Approved by
FDA
First approval
1957
1959
Drug indication
Pain
Low back pain
Parkinson disease
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 29
DESCRIPTION Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 ¦ÌM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[1][2].
PRICE 29
INDICATION Indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculo skeletal conditions.
DESCRIPTION Orphenadrine is a muscle relaxant.
Marketed formulations contain the citrate salt (PubChem CID 83823) or the hydrochloride (PubChem CID 9568).. (GtoPdb)
DESCRIPTION Orphenadrine ((¡À)-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 cytochrome P450 (CYP) 2B 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].
PRICE 53
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 ??M 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.
DESCRIPTION Orphenadrine Citrate (Flexon) is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects. (TargetMol Bioactive Compound Library)
DESCRIPTION Muscarinic acetylcholine receptor antagonist; H1 histamine receptor antagonist (LOPAC library)
DESCRIPTION A skeletal muscle relaxant used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. (BOC Sciences Bioactive Compounds)
DESCRIPTION Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. (TargetMol Bioactive Compound Library)
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. (TargetMol Bioactive Compound Library)
Cell lines
0
Organisms
1
Compound Sets
29
AdooQ Bioactive Compound Library
A11712
BOC Sciences Bioactive Compounds
orphenadrine-hydrochloride-cas-341-69-5-66545
Cayman Chemical Bioactives
26391
ChEMBL Approved Drugs
CHEMBL1200395
CHEMBL1201023
CHEMBL900
ChEMBL Drugs
CHEMBL1200395
CHEMBL1201023
CHEMBL900
CZ-OPENSCREEN Bioactive Library
DrugBank
DB01173
DrugBank Approved Drugs
DB01173
DrugCentral
1999
DrugCentral Approved Drugs
1999
DrugMAP
DMW542E
DrugMAP Approved Drugs
DMW542E
DrugMatrix
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101225
Guide to Pharmacology
7251
JUMP-MOA Compound Set
4601
Ki Database
Orphenadrine
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL900
MedChem Express Bioactive Compound Library
HY-B0369A
HY-157959
NCATS Inxight Approved Drugs
AL805O9OG9
NIH Clinical Collections (NCC)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
orphenadrine-citrate-norflex
orphenadrine-hydrochloride
TargetMol Bioactive Compound Library
T6618
T1308
T68599
The Spectrum Collection
External IDs
80
Properties
(calculated by RDKit )
Molecular Weight
269.18
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
6
Ring Count
2
Aromatic Ring Count
2
cLogP
3.66
TPSA
12.47
Fraction CSP3
0.33
Chiral centers
1.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
Muscarinic
Pathway
Neuronal Signaling
GPCR/G protein
Immunology/Inflammation
Membrane Transporter/Ion Channel
Neuroscience
Metabolic Enzyme/Protease
Target
Cholinergic
NMDA Receptor
muscarinic receptor
Sodium Channel
Cholinesterase (ChE)
Cytochrome P450
iGluR
AChR
NMDAR
H1 receptor
Noradrenaline transporter (Sodium-dependent)
MOA
acetylcholine receptor antagonist
Therapeutic Class
Antiparkinson Agents
Solubility
Soluble in DMSO
Source data