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Drug-Target Interaction

Drug

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PubChem ID:2566
Structure:
Synonyms:
(2,2-dimethyl-3H-1-benzofuran-7-yl) N-methylcarbamate
1563-66-2
2,2-Dimethyl-2,2-dihydrobenzofuranyl-7 N-methylcarbamate
2,2-dimethyl-2,3-dihydro-1-benzofuran-7-yl methylcarbamate
2,2-Dimethyl-2,3-dihydro-7-benzofuranyl N-methylcarbamate
2,2-Dimethyl-7-coumaranyl N-methylcarbamate
2,3-Dihydro-2,2-dimethyl-7-benzofuranol methylcarbamate
2,3-Dihydro-2,2-dimethyl-7-benzofuranol N-methylcarbamate
2,3-DIHYDRO-2,2-DIMETHYL-7-BENZOFURANOL, METHYLCARBAMATE
2,3-Dihydro-2,2-dimethyl-7-benzofuranyl methylcarbamate
2,3-Dihydro-2,2-dimethylbenzofuran-7-yl methylcarbamate
2,3-Dihydro-2,2-dimethylbenzofuranyl-7-N-methylcarbamate
426008_ALDRICH
45370_RIEDEL
5-17-04-00048 (Beilstein Handbook Reference)
7-Benzofuranol, 2,3-dihydro-2,2-dimethyl-, 7-(N-methylcarbamate)
7-Benzofuranol, 2,3-dihydro-2,2-dimethyl-, methylcarbamate
70143, Bayer
AC-10588
AC1L1DYQ
AI3-27164
BAY 70143
BAY 78537
Bayer 70143
BIDD:ER0379
Brifur
BRN 1428746
BSPBio_002435
c1285
C12H15NO3
C14291
C2292-59A
Carbamic acid, methyl-, 2,2-dimethyl-2,3-dihydrobenzofuran-7-yl ester
Carbamic acid, methyl-, 2,3-dihydro-2,2-dimethyl-7-benzofuranyl ester
CARBOFURAN
CARBOFURAN (PESTICIDE/FERTILIZER MIXTURE)
Carbofuran [ANSI:BSI:ISO]
Carbofurane
Caswell No. 160A
CCG-39409
CCRIS 4017
CHEBI:34611
CHEMBL416081
Chinufur
Crisfuran
Curaterr
D 1221
D002235
DivK1c_006612
EINECS 216-353-0
ENT 27,164
EPA Pesticide Chemical Code 090601
FMC 10242
Furacarb
Furadan
Furadan 3G
Furadan 4F
Furadan G
Furodan
HSDB 1530
I14-2658
Karbofuranu
Karbofuranu [Polish]
KBio1_001556
KBio2_002419
KBio2_004987
KBio2_007555
KBio3_001935
KBioGR_001155
KBioSS_002425
Kenofuran
LS-900
ME F248
Methyl carbamic acid 2,3-dihydro-2,2-dimethyl-7-benzofuranyl ester
N-Metylokarbaminian 2,3-dwuwodoro-2,2-dwumetylobenzofuranylu-7
N-Metylokarbaminian 2,3-dwuwodoro-2,2-dwumetylobenzofuranylu-7 [Polish]
NCGC00094541-01
NCGC00094541-02
NCGC00094541-03
NCGC00094541-04
NCGC00094541-05
NIA 10242
NIA-10242
NIA10242
Niagara 10242
Niagara nia-10242
NSC 167822
NSC167822
OMS 864
OMS-864
Oprea1_828936
Pillarfuran
SPBio_001742
SpecPlus_000516
Spectrum2_001871
SPECTRUM330057
Spectrum3_000848
Spectrum4_000688
Spectrum5_002012
Spectrum_001895
ST51054774
WLN: T56 BOT&J C1 C1 IOVM1
Yaltox
ZINC00056963

Target

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Uniprot ID:ACES_RAT
Synonyms:
Acetylcholinesterase
AChE
EC-Numbers:3.1.1.7
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

17188316
Neuronal oxidative injury and dendritic damage induced by carbofuran: protection by memantine.. Ramesh C Gupta; Snjezana Milatovic; Wolf-D Dettbarn; Michael Aschner; Dejan Milatovic (2007) Toxicology and applied pharmacology display abstract
Carbamate insecticides mediate their neurotoxicity by acetylcholinesterase (AChE) inactivation. Male Sprague-Dawley rats acutely intoxicated with the carbamate insecticide carbofuran (1.5 mg/kg, sc) developed hypercholinergic signs within 5-7 min of exposure, with maximal severity characterized by seizures within 30-60 min, lasting for about 2 h. At the time of peak severity, compared with controls, AChE was maximally inhibited (by 82-90%), radical oxygen species (ROS) markers (F(2)-isoprostanes, F(2)-IsoPs; and F(4)-neuroprostanes, F(4)-NeuroPs) were elevated 2- to 3-fold, and the radical nitrogen species (RNS) marker citrulline was elevated 4- to 8-fold in discrete brain regions (cortex, amygdala, and hippocampus). In addition, levels of high-energy phosphates (HEPs) were significantly reduced (ATP, by 43-56%; and phosphocreatine, by 37-48%). Values of total adenine nucleotides and total creatine compounds declined markedly (by 41-56% and 35-45%, respectively), while energy charge potential remained unchanged. Quantitative morphometric analysis of pyramidal neurons of the hippocampal CA1 region revealed significant decreases in dendritic lengths (by 64%) and spine density (by 60%). Pretreatment with the N-methyl-D-aspartate (NMDA) receptor antagonist memantine (18 mg/kg, sc), in combination with atropine sulfate (16 mg/kg, sc), significantly attenuated carbofuran-induced changes in AChE activity and levels of F(2)-IsoPs and F(4)-NeuroPs, declines in HEPs, as well as the alterations in morphology of hippocampal neurons. MEM and ATS pretreatment also protected rats from carbofuran-induced hypercholinergic behavioral activity, including seizures. These findings support the involvement of ROS and RNS in seizure-induced neuronal injury and suggest that memantine by preventing carbofuran-induced neuronal hyperactivity blocks pathways associated with oxidative damage in neurons.