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Drug-Target Interaction

Drug

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PubChem ID:3763
Structure:
Synonyms:
1-Chloro-2,2,2-trifluoroethyl difluoromethyl ether
2-Chloro-2-(difluoromethoxy)-1,1,1-trifluoroethane
2-chloro-2-difluoromethoxy-1,1,1-trifluoroethane
26675-46-7
AC-154802
AC1L1GNN
AErrane
AErrane (Veterinary)
AIDS-213021
AIDS213021
BRN 1852087
C07518
C3H2ClF5O
CCRIS 3043
CHEBI:6015
CHEMBL1256
Compound 469
D00545
D007530
DB00753
EINECS 247-897-7
Ethane, 2-chloro-2-(difluoromethoxy)-1,1,1-trifluoro-
Ether, 1-chloro-2,2,2-trifluoroethyl difluoromethyl
Forane
Forane (TN)
Forene
I14-1303
IsoFlo
Isoflurane
Isoflurane (JP15/USP/INN)
Isoflurane (JP16/USP/INN)
Isoflurane [Anaesthetics, volatile]
Isoflurane [USAN:BAN:INN:JAN]
Isoflurane [USAN:INN:BAN:JAN]
Isoflurano
Isoflurano [INN-Spanish]
Isofluranum
Isofluranum [INN-Latin]
Jsp005223
LS-7462
NCGC00181037-01
NCGC00181037-02
R-E 235dal
ST51041445
UNII-CYS9AKD70P
ATC-Codes:
Side-Effects:
Side-EffectFrequency
hepatic necrosis0.0010
hepatic failure0.0010
arrhythmia0
vomiting0
increased salivation0
nausea0
malignant hyperthermia0
jaundice0
hypotension0
hyperkalemia0
hyperglycemia0
hiccup0
hepatitis0
hallucinations0
delirium0
cough0
excitement0

Target

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Uniprot ID:NU1M_HUMAN
Synonyms:
NADH dehydrogenase subunit 1
NADH-ubiquinone oxidoreductase chain 1
EC-Numbers:1.6.5.3
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

12411515
Halothane, isoflurane and sevoflurane inhibit NADH:ubiquinone oxidoreductase (complex I) of cardiac mitochondria.. Peter J Hanley; John Ray; Ulrich Brandt; Jürgen Daut (2002) The Journal of physiology display abstract
We have investigated the effects of volatile anaesthetics on electron transport chain activity in the mammalian heart. Halothane, isoflurane and sevoflurane reversibly increased NADH fluorescence (autofluorescence) in intact ventricular myocytes of guinea-pig, suggesting that NADH oxidation was impaired. Using pig heart submitochondrial particles we found that the anaesthetics dose-dependently inhibited NADH oxidation in the order: halothane > isoflurane = sevoflurane. Succinate oxidation was unaffected by either isoflurane or sevoflurane, indicating that these agents selectively inhibit complex I (NADH:ubiquinone oxidoreductase). In addition to inhibiting NADH oxidation, halothane also inhibited succinate oxidation (and succinate dehydrogenase), albeit to a lesser extent. To test the hypothesis that complex I is a target of volatile anaesthetics, we examined the effects of these agents on NADH:ubiquinone oxidoreductase (EC 1.6.99.3) activity using the ubiquinone analogue DBQ (decylubiquinone) as substrate. Halothane, isoflurane and sevoflurane dose-dependently inhibited NADH:DBQ oxidoreductase activity. Unlike the classical inhibitor rotenone, none of the anaesthetics completely inhibited enzyme activity at high concentration, suggesting that these agents bind weakly to the 'hydrophobic inhibitory site' of complex I. In conclusion, halothane, isoflurane and sevoflurane inhibit complex I (NADH:ubiquinone oxidoreductase) of the electron transport chain. At concentrations of approximately 2 MAC (minimal alveolar concentration), the activity of NADH:ubiquinone oxidoreductase was reduced by about 20 % in the presence of halothane or isoflurane, and by about 10 % in the presence of sevoflurane. These inhibitory effects are unlikely to compromise cardiac performance at usual clinical concentrations, but may contribute to the mechanism by which volatile anaesthetics induce pharmacological preconditioning.
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