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Drug-Target Interaction

Drug

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PubChem ID:40585
Structure:
Synonyms:
(1R,3R)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropane carboxylic acid, (S)-alpha-cy ano-3-phenoxybenzyl ester
(1R-(1alpha(S*),3alpha))-3-(2,2-dibromoethenyl)-2,2-dimethyl-, cyano(3-phenoxyphenyl)methyl cyclopropanecarboxylate
(1R-(1alpha(S*),3alpha))-Cyano(3-phenoxyphenyl)methyl
(1R-(1alpha(S*),3alpha))-Cyano(3-phenoxyphenyl)methyl 3-(2,2-dibromoethenyl)-2,2-dimethylcyclopropanecarboxylate
(S)-alpha-Cyano-3-phenoxybenzyl (1R)-cis-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate
(S)-alpha-Cyano-3-phenoxybenzyl (1R,3R)-3-(2,2-dibromovinyl)-2,2-dimethyl-cyclopropan-1-carboxylate
(S)-alpha-Cyano-3-phenoxybenzyl (1R,3S)-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate
(S)-alpha-Cyano-3-phenoxybenzyl-(1R)-cis-3-(2,2-dibromovinyl)-2,2-dimethyl-cyclopropane carboxyate
(S)-cyano(3-phenoxyphenyl)methyl (1R,3R)-3-(2,2-dibromoethenyl)-2,2-dimethylcyclopropanecarboxylate
(S)-cyano[3-(phenyloxy)phenyl]methyl (1R,3R)-3-(2,2-dibromoethenyl)-2,2-dimethylcyclopropanecarboxylate
3-(2,2-Dibromoethenyl)-2,2-dimethylcyclopropanecarboxylic acid cyano(3-phenoxyphenyl)methyl ester
3-(2,2-Dibromoethenyl)-2,2-dimethylcyclopropanecarboxylic acid, cyano(3-phenoxy-phenyl)-, methyl ester
45423_FLUKA
45423_RIEDEL
45840_FLUKA
45840_RIEDEL
52918-63-5
55700-96-4
62229-77-0
Acetic anhydride
AI3-29279
alpha-Cyano-3-phenoxybenzyl (1R-(1alpha(S*),3alpha))-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate
Butoflin
Butoss
Butox
C10985
CCRIS 3704
CHEBI:4388
Cislin
Crackdown
cyano(3-phenoxyphenyl)methyl 3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate
Cyano-m-phenoxybenzyl (1R,3R)-3-(2,2-dibromovi nyl)-2,2-dimethylcyclopropanecarboxylate
Cyclopropanecarboxylic acid, 3-(2,2-dibromoethenyl)-2,2-dimethyl-, (S)-cyano(3-phenoxyphenyl)methyl ester, (1R,3R)-
Cyclopropanecarboxylic acid, 3-(2,2-dibromoethenyl)-2,2-dimethyl-, cyano(3-phenoxyphenyl)methyl ester, (1R-(1-alpha(S*),3-alpha))-
D07785
D9315_SIGMA
Decamethrin
Decamethrine
Decis
Decis 0.5ULV
Decis 1.5ULV
Decis 2.5ULV
Dekametrin (Hungarian)
Deltacide
DeltaGard
Deltagran
Deltamet hrin
Deltamethrin
Deltamethrin (BAN)
Deltamethrin solution
Deltamethrin [BSI:ISO]
Deltamethrine
Deltamethrine [ISO-French]
Deltametryna [Polish]
EINECS 258-256-6
EPA Pesticide Chemical Code 978051
Esbecythrin
FMC 45498
Glossinex 200
HSDB 6604
IPO 8831
K-Obiol
K-Othrin
K-Othrine
LS-7298
NCGC00163904-01
NCGC00163904-02
New Musigie
NRDC 161
OMS 1988
Othrin
Phagase 1
PS2071_SUPELCO
RU 22974
RUP 987
Scalibor [veterinary]
Scalibor [veterinary] (TN)
Stricker
Striker
Suspend
ZINC01532094
Zodiac
Zorcis
ATC-Codes:

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

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

References:

16169030
Characterization of deltamethrin metabolism by rat plasma and liver microsomes.. Sathanandam S Anand; James V Bruckner; Wendy T Haines; Srinivasa Muralidhara; Jeffrey W Fisher; Stephanie Padilla (2006) Toxicology and applied pharmacology display abstract
Deltamethrin, a widely used type II pyrethroid insecticide, is a relatively potent neurotoxicant. While the toxicity has been extensively examined, toxicokinetic studies of deltamethrin and most other pyrethroids are very limited. The aims of this study were to identify, characterize, and assess the relative contributions of esterases and cytochrome P450s (CYP450s) responsible for deltamethrin metabolism by measuring deltamethrin disappearance following incubation of various concentrations (2 to 400 microM) in plasma (esterases) and liver microsomes (esterases and CYP450s) prepared from adult male rats. While the carboxylesterase metabolism in plasma and liver was characterized using an inhibitor, tetra isopropyl pyrophosphoramide (isoOMPA), CYP450 metabolism was characterized using the cofactor, NADPH. Michaelis-Menten rate constants were calculated using linear and nonlinear regression as applicable. The metabolic efficiency of these pathways was estimated by calculating intrinsic clearance (Vmax/Km). In plasma, isoOMPA completely inhibited deltamethrin biotransformation at concentrations (2 and 20 microM of deltamethrin) that are 2- to 10-fold higher than previously reported peak blood levels in deltamethrin-poisoned rats. For carboxylesterase-mediated deltamethrin metabolism in plasma, Vmax=325.3+/-53.4 nmol/h/ml and Km=165.4+/-41.9 microM. Calcium chelation by EGTA did not inhibit deltamethrin metabolism in plasma or liver microsomes, indicating that A-esterases do not metabolize deltamethrin. In liver microsomes, esterase-mediated deltamethrin metabolism was completely inhibited by isoOMPA, confirming the role of carboxylesterases. The rate constants for liver carboxylesterases were Vmax=1981.8+/-132.3 nmol/h/g liver and Km=172.5+/-22.5 microM. Liver microsomal CYP450-mediated biotransformation of deltamethrin was a higher capacity (Vmax=2611.3+/-134.1 nmol/h/g liver) and higher affinity (Km=74.9+/-5.9 microM) process than carboxylesterase (plasma or liver) detoxification. Genetically engineered individual rat CYP450s (Supersomes) were used to identify specific CYP450 isozyme(s) involved in the deltamethrin metabolism. CYP1A2, CYP1A1, and CYP2C11 in decreasing order of importance quantitatively, metabolized deltamethrin. Intrinsic clearance by liver CYP450s (35.5) was more efficient than that by liver (12.0) or plasma carboxylesterases (2.4).