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Drug-Target Interaction

Drug

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PubChem ID:5335
Structure:
Synonyms:
1-Phenyl-5-sulfanilamidopyrazole
3-(p-Aminobenzenesulfonamido)-2-pheny-2H-lpyrazole
3-(p-Aminobenzenesulfonamido)-2-phenylpyrazole
4-Amino-N-(1-phenyl-1H-pyrazol-5-yl)-benzenesulfonamide
4-Amino-N-(1-phenyl-1H-pyrazol-5-yl)benzenesulfonamide
4-Amino-N-(2-phenyl-2H-pyrazol-3-yl)-benzenesulfonamide
4-amino-N-(2-phenylpyrazol-3-yl)benzenesulfonamide
5-25-09-00415 (Beilstein Handbook Reference)
5-Sulfanilamido-1-phenylpyrazole
526-08-9
AB00052218
AC1L1K4K
AIDS-059755
AIDS059755
AKOS003348743
Benzenesulfonamide, 4-amino-N-(1-phenyl-1H-pyrazol-5-yl)-
BIM-0051065.0001
BPBio1_000091
BRD-K10671814-001-05-6
BRN 0308518
BSPBio_000081
BSPBio_003442
C15H14N4O2S
CAS-526-08-9
CCG-39431
CHEBI:253330
CHEMBL1109
D013426
D01954
DB06729
Depocid
Depotsulfonamide
DivK1c_000303
Eftolon
EINECS 208-384-3
EU-0101095
Firmazolo
HMS1568E03
HMS1921J13
HMS2095E03
HMS2235J21
HMS3263K12
HMS500P05
IDI1_000303
Inamil
Isarol
Isarol V
KBio1_000303
KBio2_001886
KBio2_004454
KBio2_007022
KBio3_002662
KBioGR_000826
KBioSS_001886
Lopac-S-0758
Lopac0_001095
LS-31277
Merian
Microtan pirazolo
MLS000859612
MLS001056713
MolPort-002-070-488
N'-(1-Phenylpyrazol-5-yl)sulfanilamide
N(1)-(1-Phenylpyrazol-5-yl)sulfanilamide
N(sup 1)-(1-Phenylpyrazol-5-yl)sulfanilamide
N1-(1-Phenylpyrazol-5-yl)sulfanilamide
NCGC00015925-01
NCGC00015925-02
NCGC00015925-03
NCGC00015925-04
NCGC00015925-05
NCGC00015925-06
NCGC00015925-07
NCGC00015925-08
NCGC00015925-09
NCGC00015925-10
NCGC00094368-01
NCGC00094368-02
NCGC00094368-03
NCGC00094368-04
NCGC00094368-05
NINDS_000303
Orisul
Orisulf
Paidazolo
Phenylsulfapyrazole
Plisulfan
Prestwick0_000021
Prestwick1_000021
Prestwick2_000021
Prestwick3_000021
Prestwick_454
Raziosulfa
S 0758
S0758_SIGMA
SMR000326684
Solfafenazolo
Solfafenazolo [DCIT]
SPBio_002002
SPBio_002005
SPECTRUM1501143
Spectrum2_001943
Spectrum3_001741
Spectrum4_000443
Spectrum5_001185
Spectrum_001406
ST078027
STK663863
Sulfabid
Sulfabid (TN)
Sulfafenazol
Sulfafenazol [INN-Spanish]
Sulfafenazolo
Sulfafenazolo [Italian]
Sulfanilamide, N(sup 1)-(1-phenylpyrazol-5-yl)-
Sulfanilamide, N(sup 1)-(1-phenylpyrazol-5-yl)- (8CI)
Sulfanilamide, N1-(1-phenylpyrazol-5-yl)-
Sulfaphenazol
Sulfaphenazol [INN-French]
SULFAPHENAZOLE
Sulfaphenazole (JAN/INN)
Sulfaphenazole [INN:JAN]
Sulfaphenazolum
Sulfaphenazolum [INN-Latin]
Sulfaphenazon
Sulfaphenylpipazol
Sulfaphenylpyrazol
Sulfaphenylpyrazole
Sulphaphenazole
Sulphenazole
UC166_SIGMA
UNII-0J8L4V3F81
ZERO/006449
ZINC00057490
[(4-aminophenyl)sulfonyl](1-phenylpyrazol-5-yl)amine
ATC-Codes:

Target

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Uniprot ID:CP3A1_RAT
Synonyms:
CYPIIIA1
Cytochrome P450 3A1
P450-PCN1
EC-Numbers:1.14.14.1
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

16940989
Effects of enzyme inducers and inhibitors on the pharmacokinetics of metformin in rats: involvement of CYP2C11, 2D1 and 3A1/2 for the metabolism of metformin.. Y H Choi; M G Lee (2006) British journal of pharmacology display abstract
BACKGROUND AND PURPOSE: The types of hepatic microsomal cytochrome P450 (CYP) isozymes responsible for the metabolism of metformin in humans and rats have not been published to date. Therefore, a series of experiments using various inducers and inhibitors of CYP isozymes was conducted to find out what types of CYP isozymes are involved in the metabolism of metformin in rats. EXPERIMENTAL APPROACH: Metformin at a dose of 100 mg kg(-1) was administered intravenously to rats. The rats were pretreated with CYP inducers such as 3-methylcholanthrene, orphenadrine, isoniazid, and dexamethasone (major inducers of CYP1A1/2, 2B1/2, 2E1, and 3A1/2, respectively, in rats), or CYP inhibitors such as SKF-525 (a non-specific inhibitor of CYP isozymes), and sulfaphenazole, quinine, and troleandomycin (major inhibitors of CYP2C11, 2D1, and 3A1/2, respectively, in rats). The time-averaged non-renal clearance (CLNR) of metformin was compared with that of controls. KEY RESULTS: In rats pretreated with dexamethasone, the CLNR was significantly faster (57% increase) than for the controls. In rats pretreated with SKF-525-A, sulfaphenazole, quinine, and troleandomycin, the CLNR was significantly slower (24.3, 62.9, 77.6, and 78.7% decrease, respectively) than for the controls. However, the CLNR values did not significantly different in the rats pretreated with 3-methylencholanthrene, orphenadrine, and isoniazid compared with the controls. CONCLUSIONS AND IMPLICATIONS: Our data suggest that metformin was metabolized mainly via CYP2C11, 2D1, and 3A1/2 in rats. This result could contribute to understanding of the possible changes in metformin pharmacokinetics in disease models where CYP2C11 and/or 3A1/2 are altered.