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Identification
NameChlorzoxazone
Accession NumberDB00356  (APRD00308)
TypeSmall Molecule
GroupsApproved
Description

A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202)

Structure
Thumb
Synonyms
2-hydroxy-5-chlorobenzoxazole
5-chloro-2-Benzoxazolinone
5-chloro-2-Benzoxazolol
5-chloro-2-Benzoxazolone
5-chloro-2-Hydroxybenzoxazole
5-chloro-2(3H)-benzoxazolone
5-chloro-3H-benzooxazol-2-one
5-Chlorobenzoxazolidone
5-chlorobenzoxazolin-2-one
Chlorzoxane
Chlorzoxazon
Chlorzoxazona
Chlorzoxazone
Chlorzoxazonum
Clorzoxazona
Clorzoxazone
External Identifiers
  • MI 315
  • USAF MA-10
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Parafon Forte Dsctablet500 mg/1oralREMEDYREPACK INC.2012-11-28Not applicableUs
Parafon Forte Dsctablet500 mg/1oralJanssen Pharmaceuticals, Inc.1987-06-15Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Chlorzoxazonetablet500 mg/1oralActavis Pharma, Inc.2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1occlusive dressing techniqueDispensing Solutions, Inc.2008-12-23Not applicableUs
Chlorzoxazonetablet500 mg/1oralbryant ranch prepack2008-12-23Not applicableUs
Chlorzoxazonetablet500 mg/1oralUnit Dose Services2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralProficient Rx LP2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-04-12Not applicableUs
Chlorzoxazonetablet500 mg/1oralDIRECT RX2014-01-01Not applicableUs
Chlorzoxazonetablet375 mg/1oralMikart Inc.2010-06-01Not applicableUs
Chlorzoxazonetablet500 mg/1oralREMEDYREPACK INC.2015-11-17Not applicableUs
Chlorzoxazonetablet750 mg/1oralMikart Inc.2010-06-01Not applicableUs
Chlorzoxazonetablet500 mg/1oralClinical Solutions Wholesale2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralRebel Distributors Corp2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralA S Medication Solutions2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralPd Rx Pharmaceuticals, Inc.2008-12-23Not applicableUs
Chlorzoxazonetablet500 mg/1oralAidarex Pharmaceuticals LLC2011-08-22Not applicableUs
Chlorzoxazonetablet500 mg/1oralDispensing Solutions, Inc.2011-01-16Not applicableUs
Chlorzoxazonetablet500 mg/1oralRebel Distributors Corp1988-05-04Not applicableUs
Chlorzoxazonetablet500 mg/1oralPhysicians Total Care, Inc.1995-04-24Not applicableUs
Chlorzoxazonetablet500 mg/1oralSTAT Rx USA LLC2008-12-23Not applicableUs
Lorzonetablet750 mg/1oralVertical Pharmaceuticals, LLC2011-10-01Not applicableUs
Lorzonetablet375 mg/1oralVertical Pharmaceuticals, LLC2011-10-01Not applicableUs
Parafon Dsctablet500 mg/1oralKeltman Pharmaceuticals Inc.2004-06-20Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MyoflexinZentiva
ParaflexBioPhausia
RelaxazoneNot Available
RemularNot Available
Remular-SNot Available
SolaxinEisai
Strifon Forte DSCNot Available
Brand mixtures
NameLabellerIngredients
Acetazone ForteTeva Canada Limited
Acetazone Forte C8Teva Canada Limited
Back-aid Forte - TabRougier Pharma Division Of Ratiopharm Inc
Extra Strength Tylenol Aches and StrainsMcneil Consumer Healthcare Division Of Johnson & Johnson Inc
Gin Pain Pills - TabStella Pharmaceutical Canada Inc.
Parafon ForteMcneil Pharmaceutical, Division Of Ortho Mcneil Inc.
Parafon Forte C8 W Codeine TabMcneil Pharmaceutical, Division Of Ortho Mcneil Inc.
Parafon Forte TabletsJohnson & Johnson Merck Consumer Pharmaceuticals Of Canada
SaltsNot Available
Categories
UNIIH0DE420U8G
CAS number95-25-0
WeightAverage: 169.565
Monoisotopic: 168.993056084
Chemical FormulaC7H4ClNO2
InChI KeyInChIKey=TZFWDZFKRBELIQ-UHFFFAOYSA-N
InChI
InChI=1S/C7H4ClNO2/c8-4-1-2-6-5(3-4)9-7(10)11-6/h1-3H,(H,9,10)
IUPAC Name
5-chloro-2,3-dihydro-1,3-benzoxazol-2-one
SMILES
ClC1=CC2=C(OC(=O)N2)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzoxazolones. These are organic compounds containing a benzene fused to an oxazole ring (a five-member aliphatic ring with three carbon atoms, one oxygen atom, and one nitrogen atom) bearing a ketone group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxazoles
Sub ClassBenzoxazolones
Direct ParentBenzoxazolones
Alternative Parents
Substituents
  • Benzoxazolone
  • Chlorobenzene
  • Benzenoid
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Oxazole
  • Azole
  • Oxacycle
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the relief of discomfort associated with acute painful musculoskeletal conditions.
PharmacodynamicsChlorzoxazone, a synthetic compound, inhibits antigen-induced bronchospasms and, hence, is used to treat asthma and allergic rhinitis. Chlorzoxazone is used as an ophthalmic solution to treat conjunctivitis and is taken orally to treat systemic mastocytosis and ulcerative colitis. Chlorzoxazone is also a centrally-acting agent for painful musculoskeletal conditions. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex a.c. involved in producing and maintaining skeletal muscle spasm of varied etiology. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles.
Mechanism of actionChlorzoxazone inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. Chlorzoxazone also may reduce the release of inflammatory leukotrienes. Chlorzoxazone may act by inhibiting calcium and potassium influx which would lead to neuronal inhibition and muscle relaxation. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex arcs involved in producing and maintaining skeletal muscle spasm
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding13-18%
Metabolism

Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide.

SubstrateEnzymesProduct
Chlorzoxazone
6-hydroxychlorzoxazoneDetails
Route of eliminationChlorzoxazone is rapidly metabolized and is excreted in the urine, primarily in a conjugated form as the glucuronide.
Half lifeNot Available
ClearanceNot Available
ToxicityOral, mouse: LD50 = 440 mg/kg; Oral, rat: LD50 = 763 mg/kg; Symptoms of overdose include diarrhea, dizziness, drowsiness, headache, light-headedness, nausea, and vomiting.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.991
Caco-2 permeable+0.5
P-glycoprotein substrateNon-substrate0.8733
P-glycoprotein inhibitor INon-inhibitor0.9784
P-glycoprotein inhibitor IINon-inhibitor0.9263
Renal organic cation transporterNon-inhibitor0.9001
CYP450 2C9 substrateNon-substrate0.8243
CYP450 2D6 substrateSubstrate0.6471
CYP450 3A4 substrateNon-substrate0.5372
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9539
CYP450 2D6 inhibitorNon-inhibitor0.9338
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9522
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.7957
CarcinogenicityNon-carcinogens0.9467
BiodegradationNot ready biodegradable0.9655
Rat acute toxicity2.2388 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8675
hERG inhibition (predictor II)Non-inhibitor0.9659
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Actavis totowa llc
  • Barr laboratories inc
  • Mikart inc
  • Mutual pharmaceutical co inc
  • Ohm laboratories inc
  • Par pharmaceutical inc
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Watson laboratories inc
  • Ortho mcneil pharmaceutical inc
  • Ortho mcneil janssen pharmaceuticals inc
  • Ferndale laboratories inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tabletocclusive dressing technique500 mg/1
Tabletoral375 mg/1
Tabletoral500 mg/1
Tabletoral750 mg/1
Prices
Unit descriptionCostUnit
Parafon forte dsc 500 mg caplet2.65USD caplet
Chlorzoxazone 500 mg tablet0.87USD tablet
Chlorzoxazone 250 mg tablet0.18USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point191-191.5Marsh, D.F.; US. Patent 2,895,877; July 21, 1959; assigned to McNeil Laboratories, Inc.
water solubility1000 mg/LNot Available
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.96 mg/mLALOGPS
logP2.09ALOGPS
logP1.94ChemAxon
logS-1.8ALOGPS
pKa (Strongest Acidic)9.39ChemAxon
pKa (Strongest Basic)-2.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area38.33 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity41.07 m3·mol-1ChemAxon
Polarizability14.94 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
References
Synthesis Reference

Marsh, D.F.; US. Patent 2,895,877; July 21, 1959; assigned to McNeil Laboratories, Inc.

General References
  1. Dong DL, Luan Y, Feng TM, Fan CL, Yue P, Sun ZJ, Gu RM, Yang BF: Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. Epub 2006 Jun 29. [PubMed:16859676 ]
  2. Park JY, Kim KA, Park PW, Ha JM: Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe. J Clin Pharmacol. 2006 Jan;46(1):109-14. [PubMed:16397290 ]
  3. Wan J, Ernstgard L, Song BJ, Shoaf SE: Chlorzoxazone metabolism is increased in fasted Sprague-Dawley rats. J Pharm Pharmacol. 2006 Jan;58(1):51-61. [PubMed:16393464 ]
External Links
ATC CodesM03BB03M03BB53M03BB73
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (61.8 KB)
Interactions
Drug Interactions
Drug
AzelastineChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Chlorzoxazone.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
BuprenorphineChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DisulfiramThe metabolism of Chlorzoxazone can be decreased when combined with Disulfiram.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
EthanolChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
HydrocodoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
IsoniazidThe metabolism of Chlorzoxazone can be decreased when combined with Isoniazid.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Chlorzoxazone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
MethotrimeprazineChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineChlorzoxazone may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
MirtazapineChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
OrphenadrineChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
PramipexoleChlorzoxazone may increase the sedative activities of Pramipexole.
RopiniroleChlorzoxazone may increase the sedative activities of Ropinirole.
RotigotineChlorzoxazone may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Chlorzoxazone.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
SuvorexantChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Chlorzoxazone.
ThalidomideChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZolpidemChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Voltage-gated potassium channel activity
Specific Function:
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key ...
Gene Name:
KCNMA1
Uniprot ID:
Q12791
Molecular Weight:
137558.115 Da
References
  1. Dong DL, Luan Y, Feng TM, Fan CL, Yue P, Sun ZJ, Gu RM, Yang BF: Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. Epub 2006 Jun 29. [PubMed:16859676 ]
  2. Alvina K, Khodakhah K: KCa channels as therapeutic targets in episodic ataxia type-2. J Neurosci. 2010 May 26;30(21):7249-57. doi: 10.1523/JNEUROSCI.6341-09.2010. [PubMed:20505091 ]
  3. Syme CA, Gerlach AC, Singh AK, Devor DC: Pharmacological activation of cloned intermediate- and small-conductance Ca(2+)-activated K(+) channels. Am J Physiol Cell Physiol. 2000 Mar;278(3):C570-81. [PubMed:10712246 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Pelkonen O, Maenpaa J, Taavitsainen P, Rautio A, Raunio H: Inhibition and induction of human cytochrome P450 (CYP) enzymes. Xenobiotica. 1998 Dec;28(12):1203-53. [PubMed:9890159 ]
  2. Kurata N, Nishimura Y, Iwase M, Fischer NE, Tang BK, Inaba T, Yasuhara H: Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1. Xenobiotica. 1998 Nov;28(11):1041-7. [PubMed:9879636 ]
  3. Ernstgard L, Warholm M, Johanson G: Robustness of chlorzoxazone as an in vivo measure of cytochrome P450 2E1 activity. Br J Clin Pharmacol. 2004 Aug;58(2):190-200. [PubMed:15255802 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Wiercinska P, Squires EJ: Chlorzoxazone metabolism by porcine cytochrome P450 enzymes and the effect of cytochrome b5. Drug Metab Dispos. 2010 May;38(5):857-62. doi: 10.1124/dmd.109.030528. Epub 2010 Feb 17. [PubMed:20164110 ]
  2. Warrington JS, Court MH, Greenblatt DJ, von Moltke LL: Phenacetin and chlorzoxazone biotransformation in aging male Fischer 344 rats. J Pharm Pharmacol. 2004 Jun;56(6):819-25. [PubMed:15231049 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Yang TJ, Sai Y, Krausz KW, Gonzalez FJ, Gelboin HV: Inhibitory monoclonal antibodies to human cytochrome P450 1A2: analysis of phenacetin O-deethylation in human liver. Pharmacogenetics. 1998 Oct;8(5):375-82. [PubMed:9825829 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Shimada T, Tsumura F, Yamazaki H: Prediction of human liver microsomal oxidations of 7-ethoxycoumarin and chlorzoxazone with kinetic parameters of recombinant cytochrome P-450 enzymes. Drug Metab Dispos. 1999 Nov;27(11):1274-80. [PubMed:10534312 ]
Kind
Protein
Organism
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Gorski JC, Jones DR, Wrighton SA, Hall SD: Contribution of human CYP3A subfamily members to the 6-hydroxylation of chlorzoxazone. Xenobiotica. 1997 Mar;27(3):243-56. [PubMed:9141232 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Shimada T, Tsumura F, Yamazaki H: Prediction of human liver microsomal oxidations of 7-ethoxycoumarin and chlorzoxazone with kinetic parameters of recombinant cytochrome P-450 enzymes. Drug Metab Dispos. 1999 Nov;27(11):1274-80. [PubMed:10534312 ]
  3. Gorski JC, Jones DR, Wrighton SA, Hall SD: Contribution of human CYP3A subfamily members to the 6-hydroxylation of chlorzoxazone. Xenobiotica. 1997 Mar;27(3):243-56. [PubMed:9141232 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 04, 2014 12:03