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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:CP2E1_HUMAN
Synonyms:
4-nitrophenol 2-hydroxylase
CYPIIE1
Cytochrome P450 2E1
P450-J
EC-Numbers:1.14.13.-
1.14.13.n7
Organism:Homo sapiens
Human
PDB IDs:3E4E 3E6I
Structure:
3E6I

Binding Affinities:

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

References:

10886461
14651673
8304968
Trimethadione metabolism, a useful indicator for assessing hepatic drug-oxidizing capacity.. M Nakamura; E Tanaka; S Misawa; T Shimada; S Imaoka; Y Funae (1994) Biochemical pharmacology display abstract
The metabolism of trimethadione (TMO), a useful indicator of hepatic drug-oxidizing capacity in rats and humans, was studied using 14 different forms of rat cytochrome P450 (CYP1A1, 1A2, 2A1, 2A2, 2B1, 2B2, 2C6, 2C7, 2C11, 2C12, 2C13, 2E1, 3A2 and 4A2) and three forms of human cytochrome P450 (CYP1A2, 2C and 3A4). TMO N-demethylation was increased by treating rats with phenobarbital. CYP2C11 and 2B1 had high TMO N-demethylase activity, but 1A1 and 1A2 had low activity. Antibodies raised to CYP2C11 and 2B1/2 inhibited TMO N-demethylation in hepatic microsomes of untreated and phenobarbital-treated rats, respectively. In a reconstituted system, human CYP3A4 and 2C produced efficiently dimethadione (DMO), but CYP1A2 did not catalyse TMO N-demethylation. Antibodies raised to CYP3A2 and 2C11 inhibited TMO N-demethylation in human hepatic microsomes. These results indicated that the N-demethylation of TMO is catalysed mainly by CYP2C11 and 2B1 in rat hepatic microsomes, and that human CYP3A4 and an unspecified isoform of the 2C subfamilies contribute to TMO N-demethylation in human liver.
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.