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Identification
NameAminophenazone
Accession NumberDB01424
TypeSmall Molecule
GroupsApproved, Withdrawn
DescriptionA pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of agranulocytosis. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests. [PubChem]
Structure
Thumb
Synonyms
(Dimethylamino)phenazone
1-Phenyl-2,3-dimethyl-4-(dimethylamino)-5-pyrazolone
1-Phenyl-2,3-dimethyl-4-dimethylaminopyrazol-5-one
1,5-Dimethyl-4-dimethylamino-2-phenyl-3-pyrazolone
2,3-Dimethyl-4-dimethylamino-1-phenyl-5-pyrazolone
3-Keto-1,5-dimethyl-4-dimethylamino-2-phenyl-2,3-dihydropyrazole
4-(Dimethylamino)-1,2-dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one
4-(Dimethylamino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one
4-(Dimethylamino)antipyrine
4-Dimethylamino-1-phenyl-2,3-dimethylpyrazolone
4-Dimethylamino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one
4-Dimethylamino-2,3-dimethyl-1-phenyl-5-pyrazolone
4-Dimethylaminoantipyrine
4-Dimethylaminophenazone
Aminofenazona
Aminofenazone
Aminophenazon
Aminophenazonum
Aminopyrine
Dimethylaminoantipyrine
Dimethylaminoazophene
Dimethylaminophenazon
Dimethylaminophenazone
Dimethylaminophenyldimethylpyrazolone
Dipyrine
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII01704YP3MO
CAS number58-15-1
WeightAverage: 231.2936
Monoisotopic: 231.137162181
Chemical FormulaC13H17N3O
InChI KeyInChIKey=RMMXTBMQSGEXHJ-UHFFFAOYSA-N
InChI
InChI=1S/C13H17N3O/c1-10-12(14(2)3)13(17)16(15(10)4)11-8-6-5-7-9-11/h5-9H,1-4H3
IUPAC Name
4-(dimethylamino)-1,5-dimethyl-2-phenyl-2,3-dihydro-1H-pyrazol-3-one
SMILES
CN(C)C1=C(C)N(C)N(C1=O)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzoles
Sub ClassPyrazoles
Direct ParentPhenylpyrazoles
Alternative Parents
Substituents
  • Phenylpyrazole
  • Dialkylarylamine
  • Benzenoid
  • Pyrazolinone
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary amine
  • Lactam
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFormerly widely used as an antipyretic and analgesic in rheumatism, neuritis, and common colds. Currently used to measure total body water.
PharmacodynamicsAminophenazone is a pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of agranulocytosis. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in liver function tests. [Wikipedia]
Mechanism of actionAminophenazone is metabolized very slowly by normal newborn babies. In older infants, a higher amount of exhaled 13-CO2 is observed.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism
SubstrateEnzymesProduct
Aminophenazone
N-DesmethylaminopyrineDetails
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityCan cause life-threatening agranulocytosis.
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+0.9845
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.7772
P-glycoprotein inhibitor INon-inhibitor0.7283
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.8779
CYP450 2C9 substrateNon-substrate0.7595
CYP450 2D6 substrateSubstrate0.8154
CYP450 3A4 substrateSubstrate0.7049
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9337
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.957
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6183
Ames testAMES toxic0.6234
CarcinogenicityNon-carcinogens0.835
BiodegradationNot ready biodegradable0.9871
Rat acute toxicity2.8773 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9691
hERG inhibition (predictor II)Non-inhibitor0.7392
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point134.5 °CPhysProp
water solubility5.44E+004 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.00HANSCH,C ET AL. (1995)
logS-0.63ADME Research, USCD
Caco2 permeability-4.44ADME Research, USCD
pKa5SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility22.5 mg/mLALOGPS
logP0.94ALOGPS
logP1.15ChemAxon
logS-1ALOGPS
pKa (Strongest Basic)3.47ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area26.79 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity70.11 m3·mol-1ChemAxon
Polarizability25.87 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.35 KB)
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
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General References
  1. Rating D, Langhans CD: Breath tests: concepts, applications and limitations. Eur J Pediatr. 1997 Aug;156 Suppl 1:S18-23. [PubMed:9266210 ]
External Links
ATC CodesN02BB53N02BB03N02BB73
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Aminophenazone can be increased when it is combined with Abiraterone.
AmiodaroneThe metabolism of Aminophenazone can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Aminophenazone can be increased when it is combined with Aprepitant.
ArmodafinilThe metabolism of Aminophenazone can be decreased when combined with Armodafinil.
ArtemetherThe metabolism of Aminophenazone can be decreased when combined with Artemether.
AtazanavirThe metabolism of Aminophenazone can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Aminophenazone can be decreased when combined with Atomoxetine.
AzithromycinThe metabolism of Aminophenazone can be decreased when combined with Azithromycin.
BetaxololThe metabolism of Aminophenazone can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Aminophenazone can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Aminophenazone can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Aminophenazone can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Aminophenazone can be decreased when it is combined with Bosentan.
BupropionThe metabolism of Aminophenazone can be decreased when combined with Bupropion.
CaffeineThe metabolism of Aminophenazone can be decreased when combined with Caffeine.
CapecitabineThe metabolism of Aminophenazone can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Aminophenazone can be increased when combined with Carbamazepine.
CelecoxibThe metabolism of Aminophenazone can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Aminophenazone can be increased when it is combined with Ceritinib.
ChloramphenicolThe metabolism of Aminophenazone can be decreased when combined with Chloramphenicol.
ChloroquineThe metabolism of Aminophenazone can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Aminophenazone can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Aminophenazone can be decreased when combined with Cholecalciferol.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Aminophenazone.
CimetidineThe metabolism of Aminophenazone can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Aminophenazone can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Aminophenazone can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Aminophenazone can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Aminophenazone can be decreased when combined with Clemastine.
ClobazamThe metabolism of Aminophenazone can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Aminophenazone can be decreased when combined with Clomipramine.
ClopidogrelThe metabolism of Aminophenazone can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Aminophenazone can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Aminophenazone can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Aminophenazone can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Aminophenazone can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Aminophenazone can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Aminophenazone can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Aminophenazone can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Aminophenazone can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Aminophenazone can be decreased when it is combined with Dabrafenib.
DarifenacinThe metabolism of Aminophenazone can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Aminophenazone can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Aminophenazone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Aminophenazone can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Aminophenazone can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Aminophenazone can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Aminophenazone can be decreased when it is combined with Dexamethasone.
DihydroergotamineThe metabolism of Aminophenazone can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Aminophenazone can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Aminophenazone can be decreased when combined with Diphenhydramine.
DoxycyclineThe metabolism of Aminophenazone can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Aminophenazone can be decreased when combined with Dronedarone.
DuloxetineThe metabolism of Aminophenazone can be decreased when combined with Duloxetine.
EfavirenzThe serum concentration of Aminophenazone can be decreased when it is combined with Efavirenz.
EliglustatThe metabolism of Aminophenazone can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Aminophenazone can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Aminophenazone can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Aminophenazone can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe metabolism of Aminophenazone can be decreased when combined with Esomeprazole.
EtravirineThe serum concentration of Aminophenazone can be decreased when it is combined with Etravirine.
FelodipineThe metabolism of Aminophenazone can be decreased when combined with Felodipine.
FloxuridineThe metabolism of Aminophenazone can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Aminophenazone can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Aminophenazone can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Aminophenazone can be decreased when combined with Fluoxetine.
FluvastatinThe metabolism of Aminophenazone can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Aminophenazone can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Aminophenazone can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Aminophenazone can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Aminophenazone can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Aminophenazone can be increased when it is combined with Fusidic Acid.
GemfibrozilThe metabolism of Aminophenazone can be decreased when combined with Gemfibrozil.
HaloperidolThe metabolism of Aminophenazone can be decreased when combined with Haloperidol.
IdelalisibThe serum concentration of Aminophenazone can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Aminophenazone can be decreased when combined with Imatinib.
ImipramineThe metabolism of Aminophenazone can be decreased when combined with Imipramine.
IndinavirThe metabolism of Aminophenazone can be decreased when combined with Indinavir.
IrbesartanThe metabolism of Aminophenazone can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Aminophenazone can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Aminophenazone can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Aminophenazone can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Aminophenazone can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Aminophenazone can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Aminophenazone can be decreased when combined with Ketoconazole.
LapatinibThe metabolism of Aminophenazone can be decreased when combined with Lapatinib.
LeflunomideThe metabolism of Aminophenazone can be decreased when combined with Leflunomide.
LidocaineThe metabolism of Aminophenazone can be decreased when combined with Lidocaine.
LopinavirThe metabolism of Aminophenazone can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Aminophenazone can be decreased when combined with Lorcaserin.
LosartanThe metabolism of Aminophenazone can be decreased when combined with Losartan.
LovastatinThe metabolism of Aminophenazone can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Aminophenazone can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Aminophenazone can be decreased when it is combined with Lumacaftor.
LumefantrineThe metabolism of Aminophenazone can be decreased when combined with Lumefantrine.
MethadoneThe metabolism of Aminophenazone can be decreased when combined with Methadone.
MethotrimeprazineThe metabolism of Aminophenazone can be decreased when combined with Methotrimeprazine.
MetoprololThe metabolism of Aminophenazone can be decreased when combined with Metoprolol.
MexiletineThe metabolism of Aminophenazone can be decreased when combined with Mexiletine.
MifepristoneThe metabolism of Aminophenazone can be decreased when combined with Mifepristone.
MirabegronThe metabolism of Aminophenazone can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Aminophenazone can be decreased when it is combined with Mitotane.
MoclobemideThe metabolism of Aminophenazone can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Aminophenazone can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Aminophenazone can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Aminophenazone can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Aminophenazone can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Aminophenazone can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Aminophenazone can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Aminophenazone can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Aminophenazone can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Aminophenazone can be decreased when combined with Olaparib.
OmeprazoleThe metabolism of Aminophenazone can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Aminophenazone can be increased when it is combined with Osimertinib.
PalbociclibThe serum concentration of Aminophenazone can be increased when it is combined with Palbociclib.
PanobinostatThe metabolism of Aminophenazone can be decreased when combined with Panobinostat.
PantoprazoleThe metabolism of Aminophenazone can be decreased when combined with Pantoprazole.
ParoxetineThe metabolism of Aminophenazone can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Aminophenazone can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Aminophenazone can be increased when combined with Pentobarbital.
PhenobarbitalThe metabolism of Aminophenazone can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Aminophenazone can be increased when combined with Phenytoin.
PioglitazoneThe metabolism of Aminophenazone can be decreased when combined with Pioglitazone.
PosaconazoleThe metabolism of Aminophenazone can be decreased when combined with Posaconazole.
PrimidoneThe metabolism of Aminophenazone can be increased when combined with Primidone.
PromazineThe metabolism of Aminophenazone can be decreased when combined with Promazine.
PyrimethamineThe metabolism of Aminophenazone can be decreased when combined with Pyrimethamine.
QuinidineThe metabolism of Aminophenazone can be decreased when combined with Quinidine.
QuinineThe metabolism of Aminophenazone can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Aminophenazone can be decreased when combined with Rabeprazole.
RanolazineThe metabolism of Aminophenazone can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Aminophenazone can be increased when combined with Rifabutin.
RifampicinThe metabolism of Aminophenazone can be increased when combined with Rifampicin.
RifapentineThe metabolism of Aminophenazone can be increased when combined with Rifapentine.
RitonavirThe metabolism of Aminophenazone can be decreased when combined with Ritonavir.
RolapitantThe metabolism of Aminophenazone can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Aminophenazone can be decreased when combined with Ropinirole.
RosiglitazoneThe metabolism of Aminophenazone can be decreased when combined with Rosiglitazone.
SaquinavirThe metabolism of Aminophenazone can be decreased when combined with Saquinavir.
SecobarbitalThe metabolism of Aminophenazone can be increased when combined with Secobarbital.
SertralineThe metabolism of Aminophenazone can be decreased when combined with Sertraline.
SildenafilThe metabolism of Aminophenazone can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Aminophenazone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Aminophenazone can be increased when it is combined with Simeprevir.
SorafenibThe metabolism of Aminophenazone can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Aminophenazone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Aminophenazone can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Aminophenazone can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Aminophenazone can be decreased when combined with Sulfamethoxazole.
SulfisoxazoleThe metabolism of Aminophenazone can be decreased when combined with Sulfisoxazole.
TamoxifenThe metabolism of Aminophenazone can be decreased when combined with Tamoxifen.
TelaprevirThe metabolism of Aminophenazone can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Aminophenazone can be decreased when combined with Telithromycin.
TenofovirThe metabolism of Aminophenazone can be decreased when combined with Tenofovir.
TerbinafineThe metabolism of Aminophenazone can be decreased when combined with Terbinafine.
TeriflunomideThe serum concentration of Aminophenazone can be decreased when it is combined with Teriflunomide.
TheophyllineThe metabolism of Aminophenazone can be decreased when combined with Theophylline.
ThioridazineThe metabolism of Aminophenazone can be decreased when combined with Thioridazine.
TicagrelorThe metabolism of Aminophenazone can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Aminophenazone can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Aminophenazone can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Aminophenazone can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Aminophenazone can be decreased when combined with Tolbutamide.
TopiramateThe metabolism of Aminophenazone can be decreased when combined with Topiramate.
TranylcypromineThe metabolism of Aminophenazone can be decreased when combined with Tranylcypromine.
TrimethoprimThe metabolism of Aminophenazone can be decreased when combined with Trimethoprim.
Valproic AcidThe metabolism of Aminophenazone can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Aminophenazone can be decreased when combined with Valsartan.
VemurafenibThe serum concentration of Aminophenazone can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Aminophenazone can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Aminophenazone can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Aminophenazone can be decreased when combined with Voriconazole.
ZafirlukastThe metabolism of Aminophenazone can be decreased when combined with Zafirlukast.
ZiprasidoneThe metabolism of Aminophenazone can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 17-alpha-monooxygenase activity
Specific Function:
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty.
Gene Name:
CYP17A1
Uniprot ID:
P05093
Molecular Weight:
57369.995 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Apiwattanakul N, Sekine T, Chairoungdua A, Kanai Y, Nakajima N, Sophasan S, Endou H: Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. Mol Pharmacol. 1999 May;55(5):847-54. [PubMed:10220563 ]
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Drug created on July 24, 2007 05:44 / Updated on August 17, 2016 12:23