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Drug-Target Interaction

Drug

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PubChem ID:2206
Structure:
Synonyms:
.beta.-Antipyrine
1,2-Dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one
1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one
1,5-dimethyl-2-phenyl-2,3-dihydro-1H-pyrazol-3-one
1,5-dimethyl-2-phenylpyrazol-3-one
1-Phenyl-2,3-dimethyl-5-pyrazolone
1-Phenyl-2,3-dimethylpyrazole-5-one
10784_FLUKA
123175-91-7
2,3-Dimethyl-1-phenyl-3-pyrazolin-5-one
2,3-Dimethyl-1-phenyl-5-pyrazolone
2,3-DIMETHYL-1-PHENYLPYRAZOL-5-ONE
3-Antipyrine
3H-Pyrazol-3-one, 1,2-dihydro-1,5-dimethyl-2-phenyl-
5779-41-9
60-80-0
A4411_SIGMA
A5882_FLUKA
A5882_SIAL
AC1L1D5U
AC1Q404E
Acetasol
AF-960/00437050
AI3-15293
AIDS-020293
AIDS020293
AKOS000588788
Analgesine
Anodynin
Anodynine
Antipirin
Antipyrin
Antipyrine
Antipyrine (JP15/USP)
Antipyrine (JP16/USP)
ANTIPYRINE CRYSTALLINE
Antipyrine [JAN]
Antipyrine-3-14C
Antipyrinum
Apirelina
Auralgan
Azophen
Azophene
Azophenum
BBL001832
BIM-0051287.0001
BPBio1_000107
BRD-K46937689-001-05-1
BSPBio_000097
BSPBio_001870
C11H12N2O
C13244
CAS-60-80-0
CCG-38904
CCRIS 1369
CHEBI:31225
CHEMBL277474
component of Auralgan
D000983
D01776
DB01435
Dichloralphenazone
Dimethyloxychinizin
Dimethyloxyquinazine
DivK1c_000484
EINECS 200-486-6
Fenazon
Fenazon [Czech]
Fenazona
Fenazona [INN-Spanish]
Fenazone
HMS1568E19
HMS1920E09
HMS2091K09
HMS2095E19
HMS2272G04
HMS501I06
I14-7751
IDI1_000484
KBio1_000484
KBio2_000438
KBio2_003006
KBio2_005574
KBio3_001370
KBioGR_000624
KBioSS_000438
LS-7645
Methozin
Mixture Name
MLS001331753
MLS001332401
MLS001332402
MLS002154179
NCGC00016274-01
NCGC00016274-02
NCGC00016274-03
NCGC00016274-04
NCGC00016274-05
NCGC00016274-06
NCGC00016274-07
NCGC00094591-01
NCGC00094591-02
NCGC00094591-03
NCGC00178937-01
NCGC00178937-02
NINDS_000484
NSC 7945
NSC7945
Oxydimethylquinazine
Oxydimethylquinizine
Parodyne
Phenazon
Phenazone
Phenazone (INN)
Phenazone (pharmaceutical)
Phenazonum
Phenazonum [INN-Latin]
Phenozone
Phenylon
Phenylone
Prestwick0_000029
Prestwick1_000029
Prestwick2_000029
Prestwick3_000029
Prestwick_26
Pyramidone
Pyrazoline
Pyrazophyl
Sedatin
Sedatine
SMR000238140
SPBio_000016
SPBio_002018
SPECTRUM1500128
Spectrum2_000088
Spectrum3_000305
Spectrum4_000152
Spectrum5_000842
Spectrum_000058
ST009485
STK328171
UNII-T3CHA1B51H
WLN: T5NNVJ A1 BR& E1
ZINC00061044
ATC-Codes:

Target

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Uniprot ID:CP2CJ_HUMAN
Synonyms:
(R)-limonene 6-monooxygenase
(S)-limonene 6-monooxygenase
(S)-limonene 7-monooxygenase
CYPIIC17
CYPIIC19
Cytochrome P450 2C19
Mephenytoin 4-hydroxylase
P450-11A
P450-254C
EC-Numbers:1.14.13.48
1.14.13.49
1.14.13.80
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----

References:

8801065
Identification of the human hepatic cytochromes P450 involved in the in vitro oxidation of antipyrine.. J E Sharer; S A Wrighton (1996) Drug metabolism and disposition: the biological fate of chemicals display abstract
Antipyrine biotransformation has been used extensively in clinical studies as a marker for general hepatic oxidative or cytochrome P450 (P450)-mediated, metabolism. Studies have indicated that more than one P450 is involved in the formation of the three major human metabolites, 4-hydroxyantipyrine, norantipyrine, and 3-hydroxymethylantipyrine. However, the specific P450s involved have not yet been determined. We have developed a sensitive method for the measurement of antipyrine metabolites formed in the in vitro incubations and applied it to determine the P450s participating in the formation of each metabolite in human liver microsomes. The identification of these P450s was accomplished through the use of simple and multivariate regression analysis, selective chemical inhibitors, and microsomes containing cDNA-expressed enzymes. These methods implicated P450s 1A2, 3A, and 2A6 in the formation of 4-hydroxyantipyrine. The predominant form involved in 3-hydroxymethylantipyrine formation was found to be 1A2, although 2C9 and 2E1 seemed to participate to a lesser extent. All forms considered (1A2, 2A6, 2C9, 2C19, 2D6, 2E1, and 3A) seemed to be involved in the formation of norantipyrine, although 1A2 and 2C9 only were accepted in multivariate regression analysis. Thus, antipyrine clearance is indeed a general measure of P450 oxidative capacity, with a slight to moderate weight toward 1A2, depending on the degree of 1A2 expression. Because of the multiplicity of the enzymes involved in the formation of each metabolite, the determination of these individual metabolites would be ineffective as an indicator of the levels of specific P450 forms in human subjects.
9172960