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Drug-Target Interaction

Drug

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PubChem ID:5576
Structure:
Synonyms:
127-48-0
2,4-Oxazolidinedione, 3,5,5-trimethyl-
3,3,5-Trimethyl-2,4-diketooxazolidine
3,5,5,-Trimethyloxazolidine-2,4-dione
3,5,5-trimethyl-1,3-oxazolidine-2,4-dione
3,5,5-Trimethyl-2,4-oxazolidinedione
3,5,5-TRIMETHYL-OXAZOLIDINE-2,4-DIONE
3,5,5-Trojmetylooksazolidyno-2,4-dion
3,5,5-Trojmetylooksazolidyno-2,4-dion [Polish]
4-27-00-03237 (Beilstein Handbook Reference)
A 2297
Absentol
Absetil
AC1L1KNK
AC1Q3XZF
BPBio1_000517
BRN 0121627
BSPBio_000469
C6H9NO3
CAS-127-48-0
CHEBI:131804
CHEMBL695
Convenixa
Convexina
D00392
DB00347
Edion
EINECS 204-845-8
Epidione
Epidone
Epixal
Etydion
HMS1569H11
HMS2093D10
HMS2096H11
HMS2235E12
IRYJRGCIQBGHIV-UHFFFAOYSA-
LS-7736
Mino-Aleviatin
Minoaleuiatin
Minoaleviatin
MLS001076685
NCGC00016383-01
NCGC00016383-02
NCGC00016383-03
Neo-Absentol
NSC 15799
NSC15799
NSC169503
Petidion
Petidon
Petilep
Petimalin
Pitmal
Prestwick0_000515
Prestwick1_000515
Prestwick2_000515
Prestwick3_000515
Prestwick_815
Ptimal
SMR000499583
SPBio_002390
ST5411784
T0781_FLUKA
T0781_SIGMA
Tioxanona
Tredione
Tricione
Tridilona
Tridion
Tridione
Tridione (TN)
Tridone
Trilidona
Trimedal
Trimedone
Trimetadiona
Trimetadiona [INN-Spanish]
Trimetadione
Trimetadione [DCIT]
Trimethadion
Trimethadione
Trimethadione (JP15/INN)
Trimethadione (JP16/INN)
Trimethadione [INN:JAN]
Trimethadionum
Trimethadionum [INN-Latin]
Trimethdione
Trimethin
Trimethinum
Trimetin
Trioksal
Trioxanona
Triozanona
Tromedone
Troxidone
UNII-R7GV3H6FQ4
WLN: T5OVNV EHJ C1 E1 E1
ZINC01530710
ATC-Codes:

Target

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Uniprot ID:CP2C8_HUMAN
Synonyms:
CYPIIC8
Cytochrome P450 2C8
P450 form 1
P450 IIC2
P450 MP-12/MP-20
S-mephenytoin 4-hydroxylase
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:1PQ2 2NNH 2NNI 2NNJ 2VN0
Structure:
2VN0

Binding Affinities:

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

References:

9879636
Trimethadione metabolism by human liver cytochrome P450: evidence for the involvement of CYP2E1.. N Kurata; Y Nishimura; M Iwase; N E Fischer; B K Tang; T Inaba; H Yasuhara (1998) Xenobiotica; the fate of foreign compounds in biological systems display abstract
1. Caucasian liver samples were used in this study. N-demethylation of trimethadione (TMO) to dimethadione (DMO) was monitored in the presence of chemical inhibitors of CYPs, such as fluconazole, quinidine, dimethyl-nitrosamine, acetaminophen, phenacetin, chlorzoxazone and mephenytoin. Trimethadione N-demethylation was selectively inhibited by dimethylnitrosamine and chlorzoxazone (> 50%) and weakly inhibited by tolbutamide (12%) and fluconazole (22%), whereas other inhibitors showed no effect. This result suggested that TMO metabolism to DMO is mainly mediated by CYP2E1 and marginally by CYP2C and CYP3A4. 2. Fifteen human livers were screened and interindividual variability of TMO N-demethylation activity was 3-fold. Chlorzoxazone 6-hydroxylation activity was also measured and both activities were significantly correlated (r=0.735, p < 0.01). 3. DMO production by human cDNA expressed CYP enzymes was observed mainly for CYP2E1 (10.8 nmol/tube), marginally for CYP2C8 (0.22 nmol/tube) and not detectable for other CYP enzymes. 4. These results indicate that TMO metabolism is primarily catalysed by CYP2E1 and that trimethadione would be a suitable selective probe drug for the estimation of human CYP2E1 activity in vivo.