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Drug-Target Interaction

Drug

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PubChem ID:3562
Structure:
Synonyms:
(+-)-2-Bromo-2-chloro-1,1,1-trifluoroethane
(R)-2-Bromo-2-chloro-1,1,1-trifluoroethane
1,1,1-Trifluoro-2-bromo-2-chloroethane
1,1,1-Trifluoro-2-chloro-2-bromoethane
1-Bromo-1-chloro-2,2,2-trifluoroethane
151-67-7
16730_FLUKA
2,2,2-Trifluoro-1-chloro-1-bromoethane
2-Brom-2-chlor-1,1,1-trifluorethan
2-BROMO-2-CHLORO-1,1,1-TRIFLUOROETHANE
4-01-00-00156 (Beilstein Handbook Reference)
51230-17-2
AC1L1G7T
Alotano
Alotano [DCIT]
Anestan
B4388_SIGMA
BCQZXOMGPXTTIC-UHFFFAOYSA-
BRN 1736947
Bromchlortrifluoraethanum
Bromochlorotrifluoroethane
C07515
C2HBrClF3
CCRIS 6244
Cf3chclbr
Chalothane
CHEBI:5615
CHEMBL931
D00542
D006221
DB01159
DB02330
EINECS 205-796-5
Ethane, 1-bromo-1-chloro-2,2,2-trifluoro-
Ethane, 2-bromo-2-chloro-1,1,1-trifluoro-
Ethane, 2-bromo-2-chloro-1,1,1-trifluoro-, (+-)-
Ethane, 2-bromo-2-chloro-1,1,1-trifluoro-, (R)-
Fluktan
Fluorotane
Fluorothane
Fluothane
Fluothane (TN)
Freon 123B1
Ftorotan
Ftorotan [Russian]
Ftuorotan
Halan
Halotan
Halotano
Halotano [INN-Spanish]
Halothan
Halothane
Halothane (JP15/USP/INN)
Halothane (JP16/USP/INN)
Halothane [Anaesthetics, volatile]
Halothane [BAN:INN:JAN]
Halothane [INN:BAN:JAN]
Halothanum
Halothanum [INN-Latin]
Halsan
HMS2094K17
HSDB 6753
LS-881
Narcotan
Narcotane
Narcotann ne-spofa
Narcotann NE-spofa [Russian]
Narkotan
NCGC00090868-01
NCGC00090868-02
NCGC00090868-03
NSC 143490
NSC143490
Phthorothanum
Rhodialothan
UNII-UQT9G45D1P
WLN: GYEXFFF
ATC-Codes:
Side-Effects:
Side-EffectFrequency
arrhythmia0
cardiac arrest0
hypotension0
nausea0
vomiting0
hepatic necrosis0
respiratory arrest0

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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