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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:NOS1_RAT
Synonyms:
BNOS
Constitutive NOS
N-NOS
NC-NOS
Neuronal NOS
Nitric oxide synthase, brain
nNOS
NOS type I
EC-Numbers:1.14.13.39
Organism:Rat
Rattus norvegicus
PDB IDs:1B8Q 1F20 1K2R 1K2S 1K2T 1K2U 1LZX 1LZZ 1M00 1MMV 1MMW 1OM4 1OM5 1P6H 1P6I 1P6J 1P6K 1QAU 1QAV 1QW6 1QWC 1RS6 1RS7 1TLL 1VAG 1ZVI 1ZVL 1ZZQ 1ZZR 1ZZU 2G6H 2G6I 2G6J 2G6K 2G6L 2G6M 2G6N 2HX3 2HX4 3B3M 3B3N 3B3O 3B3P 3DQR
Structure:
3DQR

Binding Affinities:

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

References:

12105371
Tolerance against ischemic neuronal injury can be induced by volatile anesthetics and is inducible NO synthase dependent.. Krisztian J Kapinya; Diana Löwl; Carsten Fütterer; Martin Maurer; Klaus F Waschke; Nikolaj K Isaev; Ulrich Dirnagl (2002) Stroke; a journal of cerebral circulation display abstract
BACKGROUND AND PURPOSE: We tested whether volatile anesthetics induce neuroprotection that is maintained for a prolonged time. METHODS: Rats were pretreated for 3 hours with 1 minimal anesthetic concentration of isoflurane or halothane in normal air (anesthetic preconditioning [AP]). The animals were subjected to permanent middle cerebral artery occlusion (MCAO) at 0, 12, 24, or 48 hours after AP. Halothane-pretreated animals were subjected to MCAO 24 hours after AP. Histological evaluation of infarct volumes was performed 4 days after MCAO. Cerebral glucose utilization was measured 24 hours after AP with isoflurane. Primary cortical neuronal cultures were exposed to 1.4% isoflurane for 3 hours. Oxygen-glucose deprivation (OGD) was performed 24 hours after AP. Injury was assessed 24 hours later by measuring the release of lactate dehydrogenase into the medium 24 hours after OGD. RESULTS: Isoflurane anesthesia at 0, 12, and 24 hours before MCAO or halothane anesthesia 24 hours before MCAO significantly reduced infarct volumes (125+/-42 mm3, P=0.024; 118+/-51 mm3, P=0.008; 120+/-49 mm3, P=0.009; and 121+/-48 mm3, P=0.018, respectively) compared with control volumes (180+/-51 mm3). Three hours of isoflurane anesthesia in rats did not have any effect on local or mean cerebral glucose utilization measured 24 hours later. Western blot analysis from cortical extracts of AP-treated animals revealed an increase of the inducible NO synthase (iNOS) protein beginning 6 hours after AP. The iNOS inhibitor aminoguanidine (200 mg/kg IP) eliminated the infarct-sparing effect of AP. In cultured cortical neurons, isoflurane exposure 24 hours before OGD decreased the OGD-induced release of lactate dehydrogenase by 49% (P=0.002). CONCLUSIONS: Pretreatment with volatile anesthetics induces prolonged neuroprotection in vitro and in vivo, a process in which iNOS seems to be critically involved.