Identification
- Summary
Orphenadrine is a muscarinic antagonist used as an adjunct for the symptomatic relief of musculoskeletal pain and discomfort.
- Brand Names
- Norgesic, Norgesic Forte, Orfenace, Orphengesic
- Generic Name
- Orphenadrine
- DrugBank Accession Number
- DB01173
- Background
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Orphenadrine (DB01173)
- Weight
- Average: 269.3813
Monoisotopic: 269.177964363 - Chemical Formula
- C18H23NO
- Synonyms
- 2-(phenyl-o-tolylmethoxy)ethyldimethylamine
- 2-methyldiphenhydramine
- beta-Dimethylaminoethyl 2-methylbenzhydryl ether
- Dimethyl-[2-(phenyl-o-tolyl-methoxy)-ethyl]-amine
- N,N-Dimethyl-2-(alpha-2-tolylbenzoyloxy)ethylamine
- N,N-dimethyl-2-(phenyl(o-tolyl)methoxy)ethanamine
- N,N-dimethyl-2-[(o-methyl-α-phenylbenzyl)oxy]ethylamine
- o-methyldiphenhydramine
- o-monomethyldiphenhydramine
- Orfenadrina
- Orphenadrine
- Orphenadrinum
- phenyl-o-tolylmethyl dimethyaminoethyl ether
- β-dimethylaminoethyl 2-methylbenzhydryl ether
Pharmacology
- Indication
Indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute painful musculo skeletal conditions.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Back pain lower back Combination Product in combination with: Ibuprofen (DB01050) •••••••••••• Used in combination to treat Fever Combination Product in combination with: Mefenamic acid (DB00784) •••••••••••• ••••••• •••••• Used in combination to treat Menstrual cramps Combination Product in combination with: Mefenamic acid (DB00784) •••••••••••• ••••••• •••••• Used in combination to treat Mild pain Combination Product in combination with: Mefenamic acid (DB00784) •••••••••••• ••••••• •••••• Treatment of Muscle spasm •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
- Mechanism 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.
Target Actions Organism AGlutamate receptor ionotropic, NMDA 2D antagonistHumans AGlutamate receptor ionotropic, NMDA 1 antagonistHumans AGlutamate receptor ionotropic, NMDA 3B antagonistHumans AGlutamate receptor ionotropic, NMDA 3A antagonistHumans AHistamine H1 receptor antagonistHumans ASodium-dependent noradrenaline transporter inhibitorHumans USodium channel protein type 10 subunit alpha inhibitorHumans - Absorption
Orphenadrine is almost completely absorbed in the gastrointestinal tract.
- Volume of distribution
Not Available
- Protein binding
95%
- Metabolism
Biotransformation occurs mainly in the liver. Pharmacologically active metabolites are N-demethyl orphenadrine and N,N-didemethyl orphenadrine.
Hover over products below to view reaction partners
- Route of elimination
Not Available
- Half-life
13-20 hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Oral, mouse LD50 = 100 mg/kg; oral, rat LD50 = 255 mg/kg
- Pathways
Pathway Category Orphenadrine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine 1,2-Benzodiazepine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine. Abametapir The serum concentration of Orphenadrine can be increased when it is combined with Abametapir. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Orphenadrine. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Orphenadrine. Acebutolol The metabolism of Acebutolol can be decreased when combined with Orphenadrine. - Food Interactions
- Avoid alcohol.
- Take with or without food. Food does not significantly affect absorption.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Orphenadrine citrate X0A40N8I4S 4682-36-4 MMMNTDFSPSQXJP-UHFFFAOYSA-N Orphenadrine hydrochloride UBY910DUXH 341-69-5 UQZKYYIKWZOKKD-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Antiflex / Banflex / Biorphen / Disipal / Flexoject / Mio-Rel / OrfenAce / Orfro
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Disipal Tab 50mg Tablet 50 mg Oral 3 M Pharmaceuticals, A Division Of 3 M Canada Company 1957-12-31 2002-07-09 Canada 
Norflex Injection 60 mg/2mL Intramuscular; Intravenous 3M Company 1960-10-02 2006-12-29 US 
Norflex Tablet, extended release 100 mg/1 Oral Physicians Total Care, Inc. 1995-04-06 2011-05-31 US Norflex Liquid 30 mg / mL Intramuscular; Intravenous Valeant Canada Lp Valeant Canada S.E.C. 1961-12-31 2014-07-30 Canada Norflex Tablet, extended release 100000 ug/1 Oral 3M Company 1959-11-04 2006-12-29 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Orphenadrine Citrate Tablet, extended release 100 mg/1 Oral RedPharm Drug, Inc. 1998-06-19 Not applicable US Orphenadrine Citrate Tablet, extended release 100 mg/1 Oral Rebel Distributors 1998-06-19 Not applicable US 
Orphenadrine Citrate Tablet, extended release 100 mg/1 Oral Clinical Solutions Wholsesale 1998-06-19 2017-06-26 US 
Orphenadrine Citrate Tablet, extended release 100 mg/1 Oral Proficient Rx LP 2000-02-15 Not applicable US Orphenadrine Citrate Tablet, extended release 100 mg/1 Oral H.J. Harkins Company 2000-06-23 Not applicable US 
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Norflex Tablet, extended release 100 mg Oral Valeant Canada Lp Valeant Canada S.E.C. 1993-12-31 2014-07-30 Canada Orfenace Tablet 100mg Tablet 100 mg Oral Sterimax Inc 1994-12-31 Not applicable Canada Sandoz Orphenadrine Tablet, extended release 100 mg Oral Sandoz Canada Incorporated 2001-02-27 Not applicable Canada นอร์เฟลก Tablet, delayed release 100 mg บริษัท ไอโนวา ฟาร์มา (ประเทศไทย) จำกัด 2018-04-03 Not applicable Thailand 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ANAREX TABLETS Orphenadrine citrate (35 mg) + Acetaminophen (450 mg) Tablet Oral BEACONS PHARMACEUTICALS PTE. LTD. 1991-03-30 Not applicable Singapore 
CAMGESIC TABLET Orphenadrine citrate (35 mg) + Acetaminophen (450 mg) Tablet Oral PHARMATECH RESOURCES (FE) PTE. LTD. 1998-02-07 Not applicable Singapore CETAGESIC TABLET Orphenadrine citrate (25 mg) + Acetaminophen (500 mg) Tablet Oral DUOPHARMA (SINGAPORE) PTE LTD 1991-04-22 Not applicable Singapore CORILAX PINK Orphenadrine citrate (35 mg) + Acetaminophen (450 mg) Tablet Oral บริษัท ชุมชนเภสัชกรรม จำกัด (มหาชน) 2004-03-17 Not applicable Thailand MERA Orphenadrine citrate (35 mg) + Acetaminophen (500 mg) Tablet Oral บริษัท อินแพคฟาร์มา จำกัด 2002-03-22 Not applicable Thailand - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Norflex Orphenadrine citrate (100 mg/1) Tablet, extended release Oral Physicians Total Care, Inc. 1995-04-06 2011-05-31 US
Categories
- ATC Codes
- M03BC51 — Orphenadrine, combinations
- M03BC — Ethers, chemically close to antihistamines
- M03B — MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
- M03 — MUSCLE RELAXANTS
- M — MUSCULO-SKELETAL SYSTEM
- N04AB — Ethers chemically close to antihistamines
- N04A — ANTICHOLINERGIC AGENTS
- N04 — ANTI-PARKINSON DRUGS
- N — NERVOUS SYSTEM
- Drug Categories
- Agents producing tachycardia
- Amines
- Anti-Dyskinesia Agents
- Anti-Parkinson Drugs
- Anticholinergic Agents
- Autonomic Agents
- Benzene Derivatives
- Benzhydryl Compounds
- Central Nervous System Agents
- Central Nervous System Depressants
- Centrally-mediated Muscle Relaxation
- Cholinergic Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strong)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strong)
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Ethers, Chemically Close to Antihistamines
- Ethylamines
- Histamine Antagonists
- Histamine H1 Antagonists
- Miscellaneous Skeletal Muscle Relaxants
- Muscarinic Antagonists
- Muscle Relaxants
- Muscle Relaxants, Centrally Acting Agents
- Musculo-Skeletal System
- Nervous System
- Neurotransmitter Agents
- NMDA Receptor Antagonists
- Parasympatholytics
- Peripheral Nervous System Agents
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylmethanes
- Direct Parent
- Diphenylmethanes
- Alternative Parents
- Benzylethers / Toluenes / Trialkylamines / Dialkyl ethers / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Amine / Aromatic homomonocyclic compound / Benzylether / Dialkyl ether / Diphenylmethane / Ether / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organonitrogen compound
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- tertiary amino compound, ether (CHEBI:7789)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- AL805O9OG9
- CAS number
- 83-98-7
- InChI Key
- QVYRGXJJSLMXQH-UHFFFAOYSA-N
- InChI
- InChI=1S/C18H23NO/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
- IUPAC Name
- dimethyl({2-[(2-methylphenyl)(phenyl)methoxy]ethyl})amine
- SMILES
- CN(C)CCOC(C1=CC=CC=C1)C1=CC=CC=C1C
References
- General References
- 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. [Article]
- External Links
- Human Metabolome Database
- HMDB0015304
- KEGG Drug
- D08305
- KEGG Compound
- C07935
- PubChem Compound
- 4601
- PubChem Substance
- 46506085
- ChemSpider
- 4440
- BindingDB
- 50062614
- 7715
- ChEBI
- 7789
- ChEMBL
- CHEMBL900
- Therapeutic Targets Database
- DAP000858
- PharmGKB
- PA450715
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Orphenadrine
- FDA label
- Download (247 KB)
- MSDS
- Download (73.6 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Supportive Care Pain Management / Posterior Spinal Fusion 1 4 Completed Treatment Back Pain Lower Back 1 4 Completed Treatment Pain / Postoperative pain 1 4 Completed Treatment Unilateral Knee Arthroplasty 1 4 Unknown Status Supportive Care Colon Cancer / Colon Diverticulosis / Colon Neoplasm / Constipation / Diverticulitis, Colonic / Drug Induced Constipation / Ileus / Ileus; Mechanical / Paralytic Ileus / Postoperative pain / Rectal Cancer / Rectal Neoplasms 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Abraxis BioScience Inc.
- Actavis Group
- Aidarex Pharmacuticals LLC
- Alba Pharmacal
- A-S Medication Solutions LLC
- Avkare Incorporated
- Bedford Labs
- Ben Venue Laboratories Inc.
- Bryant Ranch Prepack
- Clint Pharmaceutical Inc.
- Corepharma LLC
- DispenseXpress Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Eon Labs
- Gallipot
- Gavis Pharmaceuticals LLC
- Global Pharmaceuticals
- Graceway Pharmaceuticals
- H.J. Harkins Co. Inc.
- Impax Laboratories Inc.
- Innoviant Pharmacy Inc.
- International Ethical Labs Inc.
- Kiel Laboratories Inc.
- Lake Erie Medical and Surgical Supply
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharma Pac LLC
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepak Systems Inc.
- Rebel Distributors Corp.
- Redpharm Drug
- Resource Optimization and Innovation LLC
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- St Mary's Medical Park Pharmacy
- Stat Rx Usa
- Watson Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral 35 mg Tablet Oral 25 mg Tablet, coated Oral 50 MG Solution Parenteral 60.00 mg Solution Parenteral Injection Intramuscular; Intravenous 60 mg/2mL Liquid Intramuscular; Intravenous 30 mg / mL Tablet, extended release Oral 100 mg/1 Tablet, extended release Oral 100000 ug/1 Tablet Oral Capsule Oral Tablet, film coated Oral 250 mg Injection Intramuscular; Intravenous 30 mg/1mL Injection, solution Intramuscular; Intravenous 30 mg/1mL Tablet Oral 100 mg/1 Tablet Oral Tablet, multilayer Oral Solution Parenteral 60.000 mg Tablet, extended release Oral 100 mg Tablet, delayed release 100 mg Tablet, film coated Tablet Oral 70 mg Tablet, film coated 100 mg Tablet, coated Oral Tablet Oral 100 mg Tablet Oral 50 mg - Prices
Unit description Cost Unit Norflex 30 mg/ml ampul 14.31USD ml Orphenadrine 30 mg/ml ampule 11.25USD ml Orphenadrine Compound-DS 50-770-60 mg tablet 2.94USD tablet Orphenadrine comp forte tablet 2.84USD tablet Norflex er 100 mg tablet 2.67USD tablet Norflex 100 mg tablet sa 2.64USD tablet Orphenadrine Citrate CR 100 mg 12 Hour tablet 2.26USD tablet Orphenadrine er 100 mg tablet 2.17USD tablet Orphenadrine citrate powder 1.6USD g Orphenadrine comp tablet 1.31USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) < 25 °C PhysProp boiling point (°C) 195 °C at 1.20E+01 mm Hg PhysProp water solubility Sparingly soluble in water Not Available logP 3.77 SANGSTER (1993) pKa 8.91 SANGSTER (1994) - Predicted Properties
Property Value Source Water Solubility 0.03 mg/mL ALOGPS logP 3.5 ALOGPS logP 4.17 Chemaxon logS -4 ALOGPS pKa (Strongest Basic) 8.87 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 12.47 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 84.97 m3·mol-1 Chemaxon Polarizability 31.83 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9881 Blood Brain Barrier + 0.9134 Caco-2 permeable + 0.8654 P-glycoprotein substrate Substrate 0.6196 P-glycoprotein inhibitor I Inhibitor 0.5825 P-glycoprotein inhibitor II Non-inhibitor 0.6378 Renal organic cation transporter Inhibitor 0.7359 CYP450 2C9 substrate Non-substrate 0.7658 CYP450 2D6 substrate Substrate 0.8918 CYP450 3A4 substrate Substrate 0.6958 CYP450 1A2 substrate Non-inhibitor 0.6363 CYP450 2C9 inhibitor Non-inhibitor 0.9191 CYP450 2D6 inhibitor Inhibitor 0.8949 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.9363 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5979 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.6341 Biodegradation Not ready biodegradable 0.9422 Rat acute toxicity 2.8405 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5224 hERG inhibition (predictor II) Inhibitor 0.7052
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 169.6026427 predictedDarkChem Lite v0.1.0 [M-H]- 160.14406 predictedDeepCCS 1.0 (2019) [M+H]+ 169.6315427 predictedDarkChem Lite v0.1.0 [M+H]+ 162.50206 predictedDeepCCS 1.0 (2019) [M+Na]+ 169.8909427 predictedDarkChem Lite v0.1.0 [M+Na]+ 168.5952 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Nmda glutamate receptor activity
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine.
- Gene Name
- GRIN2D
- Uniprot ID
- O15399
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 2D
- Molecular Weight
- 143750.685 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Voltage-gated cation channel activity
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic p...
- Gene Name
- GRIN1
- Uniprot ID
- Q05586
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 1
- Molecular Weight
- 105371.945 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Nmda glutamate receptor activity
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine.
- Gene Name
- GRIN3B
- Uniprot ID
- O60391
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 3B
- Molecular Weight
- 112990.98 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein phosphatase 2a binding
- Specific Function
- NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May ...
- Gene Name
- GRIN3A
- Uniprot ID
- Q8TCU5
- Uniprot Name
- Glutamate receptor ionotropic, NMDA 3A
- Molecular Weight
- 125464.07 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Kornhuber J, Parsons CG, Hartmann S, Retz W, Kamolz S, Thome J, Riederer P: 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Histamine receptor activity
- Specific Function
- In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
- Gene Name
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Rumore MM, Schlichting DA: Analgesic effects of antihistaminics. Life Sci. 1985 Feb 4;36(5):403-16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Norepinephrine:sodium symporter activity
- Specific Function
- Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Pubill D, Canudas AM, Pallas M, Sureda FX, Escubedo E, Camins A, Camarasa J: Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity
- Specific Function
- Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference acro...
- Gene Name
- SCN10A
- Uniprot ID
- Q9Y5Y9
- Uniprot Name
- Sodium channel protein type 10 subunit alpha
- Molecular Weight
- 220623.605 Da
References
- Pubill D, Canudas AM, Pallas M, Sureda FX, Escubedo E, Camins A, Camarasa J: Assessment of the adrenergic effects of orphenadrine in rat vas deferens. J Pharm Pharmacol. 1999 Mar;51(3):307-12. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Peng FC, Lin Wu SW: Metabolism of territrem a in liver microsomes from male wistar rats: 3. Cytochrome p-450 isoforms catalyzing tra metabolism. J Toxicol Environ Health A. 2002 Dec 27;65(24):2163-75. [Article]
- Lin Wu SW, Jean WC, Peng FC, Edwards RJ: Cytochrome P-4503A1 catalyzes the formation of MA1 from territrem a in liver microsomes of 7-week-old female Wistar rats. J Toxicol Environ Health A. 2003 Mar 14;66(5):453-67. [Article]
- Chang TK, Weber GF, Crespi CL, Waxman DJ: Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes. Cancer Res. 1993 Dec 1;53(23):5629-37. [Article]
- Stresser DM, Dehal SS, Kupfer D: Ring hydroxylation of [o-3H]methoxychlor as a probe for liver microsomal CYP2B activity: potential for in vivo CYP2B assay. Anal Biochem. 1996 Jan 1;233(1):100-7. [Article]
- Murray M, Fiala-Beer E, Sutton D: Upregulation of cytochromes P450 2B in rat liver by orphenadrine. Br J Pharmacol. 2003 Jun;139(4):787-96. [Article]
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
- Guo Z, Raeissi S, White RB, Stevens JC: Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Drug Metab Dispos. 1997 Mar;25(3):390-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Roos PH, Mahnke A: Metabolite complex formation of orphenadrine with cytochrome P450. Involvement of CYP2C11 and CYP3A isozymes. Biochem Pharmacol. 1996 Jul 12;52(1):73-84. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Sai Y, Dai R, Yang TJ, Krausz KW, Gonzalez FJ, Gelboin HV, Shou M: Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica. 2000 Apr;30(4):327-43. [Article]
- Sutrisna E: The Impact of CYP1A2 and CYP2E1 Genes Polymorphism on Theophylline Response. J Clin Diagn Res. 2016 Nov;10(11):FE01-FE03. doi: 10.7860/JCDR/2016/21067.8914. Epub 2016 Nov 1. [Article]
- Ekins S, VandenBranden M, Ring BJ, Wrighton SA: Examination of purported probes of human CYP2B6. Pharmacogenetics. 1997 Jun;7(3):165-79. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Data supported only by in vitro evidence.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Guo Z, Raeissi S, White RB, Stevens JC: Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Drug Metab Dispos. 1997 Mar;25(3):390-3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- Guo Z, Raeissi S, White RB, Stevens JC: Orphenadrine and methimazole inhibit multiple cytochrome P450 enzymes in human liver microsomes. Drug Metab Dispos. 1997 Mar;25(3):390-3. [Article]
- Murray M, Fiala-Beer E, Sutton D: Upregulation of cytochromes P450 2B in rat liver by orphenadrine. Br J Pharmacol. 2003 Jun;139(4):787-96. [Article]
- Svensson US, Ashton M: Identification of the human cytochrome P450 enzymes involved in the in vitro metabolism of artemisinin. Br J Clin Pharmacol. 1999 Oct;48(4):528-35. doi: 10.1046/j.1365-2125.1999.00044.x. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- BinderRegulator
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Martinez-Gomez MA, Carril-Aviles MM, Sagrado S, Villanueva-Camanas RM, Medina-Hernandez MJ: Characterization of antihistamine-human serum protein interactions by capillary electrophoresis. J Chromatogr A. 2007 Apr 20;1147(2):261-9. doi: 10.1016/j.chroma.2007.02.054. Epub 2007 Feb 22. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54