Aminophenazone

Identification

Summary

Aminophenazone is an analgesic drug used to treat acute migraine attacks in combination with ergotamine and caffeine.

Generic Name
Aminophenazone
DrugBank Accession Number
DB01424
Background

Aminophenazone is a pyrazolone with analgesic, anti-inflammatory, and antipyretic properties that carries a risk of agranulocytosis. In biomedical applications, radiolabelled (13C-labeled) aminophenazone has been used in breath tests to measure the cytochrome P-450 metabolic activity in liver function tests. The FDA suspended the use of aminophenazone due to its association with agranulocytosis, a life-threatening side effect.2,3

Type
Small Molecule
Groups
Approved, Withdrawn
Structure
Weight
Average: 231.2936
Monoisotopic: 231.137162181
Chemical Formula
C13H17N3O
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
  • Aminophenazone
  • Aminophenazonum
  • Aminopyrine
  • Dimethylaminoantipyrine
  • Dimethylaminoazophene
  • Dimethylaminophenazon
  • Dimethylaminophenazone
  • Dimethylaminophenyldimethylpyrazolone
  • Dipyrine
External IDs
  • NSC-4993

Pharmacology

Indication

Formerly widely used as an antipyretic and analgesic in rheumatism, neuritis, and common colds. Currently used to measure total body water.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination for symptomatic treatment ofAcute migraineCombination Product in combination with: Caffeine (DB00201), Ergotamine (DB00696)•••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Aminophenazone exhibits analgesic, anti-inflammatory, and antipyretic properties.

Mechanism of action

Aminophenazone is metabolized very slowly by normal newborn babies. In older infants, a higher amount of exhaled 13-CO2 is observed.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hover over products below to view reaction partners

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Can cause life-threatening agranulocytosis.

Pathways
Not Available
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.
DrugInteraction
AbacavirAminophenazone may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbametapirThe serum concentration of Aminophenazone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Aminophenazone can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding and hemorrhage can be increased when Aminophenazone is combined with Abciximab.
AbirateroneThe serum concentration of Aminophenazone can be increased when it is combined with Abiraterone.
Food Interactions
Not Available

Products

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
VIRDEXAminophenazone (250 MG) + Caffeine (100 MG) + Ergotamine tartrate (2 MG)SuppositoryRectalFulton Medicinali S.P.A.2014-07-08Not applicableItaly flag
VIRDEXAminophenazone (250 MG) + Caffeine (100 MG) + Ergotamine tartrate (0.5 MG)SuppositoryRectalFulton Medicinali S.P.A.2014-07-08Not applicableItaly flag

Categories

ATC Codes
N02BB53 — Aminophenazone, combinations excl. psycholepticsN02BB03 — AminophenazoneN02BB73 — Aminophenazone, combinations with psycholeptics
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Azoles
Sub Class
Pyrazoles
Direct Parent
Phenylpyrazoles
Alternative Parents
Dialkylarylamines / Pyrazolones / Benzene and substituted derivatives / Vinylogous amides / Heteroaromatic compounds / Lactams / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organic oxides
show 1 more
Substituents
Amine / Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Dialkylarylamine / Heteroaromatic compound / Hydrocarbon derivative / Lactam / Monocyclic benzene moiety / Organic nitrogen compound
show 10 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
tertiary amino compound, pyrazolone (CHEBI:160246)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
01704YP3MO
CAS number
58-15-1
InChI Key
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

References

General References
  1. Rating D, Langhans CD: Breath tests: concepts, applications and limitations. Eur J Pediatr. 1997 Aug;156 Suppl 1:S18-23. [Article]
  2. Chan TY, Chan AW: Aminopyrine-induced blood dyscrasias--still a problem in many parts of the world. Pharmacoepidemiol Drug Saf. 1996 Jul;5(4):215-9. doi: 10.1002/(SICI)1099-1557(199607)5:4<215::AID-PDS208>3.0.CO;2-5. [Article]
  3. Code of Federal Regulations 216.24: Drug products withdrawn or removed from the market for reasons of safety or effectiveness. [Link]
Human Metabolome Database
HMDB0015493
KEGG Drug
D00556
KEGG Compound
C07539
PubChem Compound
6009
PubChem Substance
46504975
ChemSpider
5787
BindingDB
74258
RxNav
695
ChEBI
160246
ChEMBL
CHEMBL288470
ZINC
ZINC000000057115
PharmGKB
PA164748135
Wikipedia
Aminophenazone

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
SolutionOral
SuppositoryRectal
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134.5 °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)3.66Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count3Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area26.79 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity70.11 m3·mol-1Chemaxon
Polarizability25.86 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
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)

Spectra

Mass Spec (NIST)
Download (8.35 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0159-4970000000-8cb60fc41366bf1c7f80
GC-MS Spectrum - EI-BGC-MSsplash10-053s-9250000000-c3308b81b44067a47f7e
GC-MS Spectrum - EI-BGC-MSsplash10-0a4i-9100000000-40e7051a3536ae680d1a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dr-1900000000-49de43a88698c1df262b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0190000000-d7bfbe39ac8d423c5cfd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03e9-4940000000-243b2713c256a2ab8b6c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dj-9700000000-3ef4e69c38623bfd699f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-06r2-9300000000-762e3df6382a5e2052a3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0592-9100000000-b9c175ecf48888c0267a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4j-9100000000-9fa64e7904c1473d9d32
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-0290000000-27bac0f1542859b73671
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03e9-4940000000-a4c3f3e347d595ad803e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dj-9700000000-ac217c24c44682808465
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-06xt-9300000000-f8259f5a45014efc58ee
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052b-9100000000-307762c9c387df2fcbf4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4j-9100000000-3c5267564fda210cc134
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dr-1900000000-ab951ea405c6154ef630
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-001i-0090000000-2527cae3cd95916624e4
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-3910000000-f7ee26001f3fbe463bae
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-01vk-9400000000-243fad64356c2d2c4864
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0592-9100000000-bbc78ee3e540bd560a88
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0aba-9000000000-1c4e7d6f8c8bbdc08335
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-03di-1900000000-82e0b1220cb4b6d7a2cf
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01ot-9600000000-fb0b4ca3e97bcda1fda4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-9200000000-2d261a76cbc47734fb79
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dr-1900000000-3a05afb5d5b85cbb3974
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dr-1900000000-16e77429b30962ec17d5
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01q9-2950000000-72b3f0db0bdfe8167dea
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-0090000000-4137c02cde71ee3e88cc
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-0090000000-93f0f32b70d4b1b327a5
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-001i-9360000000-d54103c1140ff8844d5c
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-2390000000-e3498098f53e21d913ae
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-05x3-9100000000-300a543f90c9c3cb85da
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-00kf-9310000000-56eebc1daa9ef58655d5
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-161.911232
predicted
DarkChem Lite v0.1.0
[M-H]-154.737173
predicted
DarkChem Lite v0.1.0
[M-H]-162.291932
predicted
DarkChem Lite v0.1.0
[M-H]-158.22194
predicted
DeepCCS 1.0 (2019)
[M+H]+163.105332
predicted
DarkChem Lite v0.1.0
[M+H]+158.8144779
predicted
DarkChem Lite v0.1.0
[M+H]+163.035732
predicted
DarkChem Lite v0.1.0
[M+H]+160.57994
predicted
DeepCCS 1.0 (2019)
[M+Na]+162.397032
predicted
DarkChem Lite v0.1.0
[M+Na]+165.2300379
predicted
DarkChem Lite v0.1.0
[M+Na]+166.6731
predicted
DeepCCS 1.0 (2019)

Enzymes

Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
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. [Article]
  2. 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]
  3. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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. [Article]
  2. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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. [Article]
  2. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C18
Uniprot ID
P33260
Uniprot Name
Cytochrome P450 2C18
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. [Article]
  2. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
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 ...
Gene Name
CYP17A1
Uniprot ID
P05093
Uniprot Name
Steroid 17-alpha-hydroxylase/17,20 lyase
Molecular Weight
57369.995 Da
References
  1. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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. [Article]
  2. Niwa T, Tsutsui M, Kishimoto K, Yabusaki Y, Ishibashi F, Katagiri M: Inhibition of drug-metabolizing enzyme activity in human hepatic cytochrome P450s by bisphenol A. Biol Pharm Bull. 2000 Apr;23(4):498-501. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data for this enzyme action is limited to an in vitro study.
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
  1. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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. [Article]
  2. Niwa T, Sato R, Yabusaki Y, Ishibashi F, Katagiri M: Contribution of human hepatic cytochrome P450s and steroidogenic CYP17 to the N-demethylation of aminopyrine. Xenobiotica. 1999 Feb;29(2):187-93. doi: 10.1080/004982599238731 . [Article]

Transporters

Kind
Protein
Organism
Humans
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 ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
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. [Article]

Drug created at July 24, 2007 11:44 / Updated at November 11, 2022 16:49