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Drug-Target Interaction

Drug

show drug details
PubChem ID:3406
Structure:
Synonyms:
1H-Pyrazole, 4-methyl-
222569_ALDRICH
4-methyl-1H-pyrazole
4-Methylpyrazol
4-Methylpyrazole
4-Methylpyrazole hydrochloride
4PZ
5-23-05-00031 (Beilstein Handbook Reference)
7554-65-6
AC-4833
AC1L1FV5
AC1Q2OK9
AC1Q2OKA
AG-H-00685
AG-H-01096
AKOS000265586
Antizol
Antizol (TN)
BRN 0105204
C07837
C4H6N2
CCG-204808
CHEBI:5141
CHEMBL1308
CPD0-1652
D00707
DB01213
EINECS 231-445-0
Fomepizol
Fomepizol [INN-Spanish]
Fomepizole
Fomepizole (USAN/INN)
Fomepizole [USAN:INN]
Fomepizolum
Fomepizolum [INN-Latin]
I11-0350
Lopac-M-1387
Lopac0_000723
LS-128524
M0774
MLS001335923
MLS002153469
NCGC00015646-01
NCGC00015646-02
NCGC00015646-03
NCGC00162231-01
PYRAZOLE, 4-METHYL-
S14-0570
SBB004402
SMR000059088
SMR000326764
STK256626
TL8005172
UNII-83LCM6L2BY
ZINC00897288
ATC-Codes:
Side-Effects:
Side-EffectFrequency
abdominal pain0
nausea0
nystagmus0
pain0
pharyngitis0
phlebitis0
seizures0
shock0
tachycardia0
vertigo0
vomiting0
sinus bradycardia0
agitation0
lightheadedness0
blurred vision0
bradycardia0
lymphangitis0
low back pain0
hypotension0
drunk0
anemia0
anxiety0
back pain0
diarrhea0
dizziness0
somnolence0
dyspepsia0
eosinophilia0
rash0
fever0
flushing0
headache0
heartburn0
hiccup0
feeling drunk0

Target

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Uniprot ID:Q6P9U7_RAT
Synonyms:
L-lactate dehydrogenase
EC-Numbers:1.1.1.27
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

11407538
Bioactivation to free radicals and cytotoxicity of 1,1-dichloro-1-fluoroethane (HCFC-141b).. A Zanovello; R Tolando; R Ferrara; S Bortolato; M Manno (2001) Xenobiotica; the fate of foreign compounds in biological systems display abstract
1. The in vitro bioactivation by rat liver microsomes and the cytotoxicity in rat hepatocytes of 1,1-dichloro-1-fluoroethane (HCFC-141b), a replacement for some ozone depleting chlorofluorocarbons (CFC), have been investigated. 2. Anaerobic incubations of liver microsomes from pyridine-induced rats with HCFC-141b in the presence of the spin-trapping agent N-t-butyl-alpha-phenylnitrone (PBN) resulted in the formation of a typical ESR radical signal. 3. In the presence of HCFC-141b, a dose-dependent formation of conjugated dienes was observed that was partially inhibited by PBN, glutathione (GSH) and vitamin C. Moreover, HCFC-141b increased the release of lactate dehydrogenase (LDH) and the depletion of cellular glutathione in isolated rat hepatocytes under both normoxic and hypoxic conditions. 4. HCFC-141b-dependent cytotoxicity was completely prevented by PBN under both conditions and it was partially prevented under normoxic conditions by the broad-spectrum P450 inhibitor metyrapone, the P4502E1 specific inhibitor 4-methylpyrazole and the P4503A-specific inhibitor troleandomycin. Interestingly, HCFC-141b-dependent glutathione depletion was not prevented by PBN, metyrapone, 4-methylpyrazole or troleandomycin, whereas two glutathione depletors, 2,6-dimethyl-2,5-heptadien-4-one (phorone) and diethylmaleate, partially prevented LDH release. 5. The present results indicate that HCFC-141b is reductively metabolized in vitro to free radical intermediates by P450, in particular by the CYP2E1 and, to a lower extent, CYP3A isoforms, leading to peroxidative membrane damage and glutathione-independent cytotoxicity.