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In vitro covalent binding of cismethrin, bioresmethrin, and their common alcohol to hepatic proteins

Journal Article · · Toxicol. Appl. Pharmacol.; (United States)
; ; ; ; ;

When (/sup 14/C)Alcohol-labeled cismethrin, bioresmethrin, and 5-benzyl-3-furylmethyl alcohol (BFA) were incubated with rat liver S 9 homogenates or microsomes, a proportion of the radioactive compounds was covalently bound to proteins. The covalent binding was greater with phenobarbital-pretreated rats, and dependent on a NADPH-generating system. When a S 9 homogenate was used, the bound compounds were two times higher for cismethrin than for bioresmethrin and BFA. Inversely, when microsomes were used more covalent binding occurred with bioresmethrin and BFA than with cismethrin. The inhibition of esterases by tetraethyl pyrophosphate (TEPP) in a S 9 homogenate did not alter the amount of covalent binding to the three compounds whereas malathion inhibited this binding. Treatment of a S 9 homogenate with piperonyl butoxide, however, greatly reduced covalent binding. Covalent binding was inhibited when the microsomes were incubated with carbon monoxide or modified by thermal denaturation. It is suggested that oxidative metabolism was responsible for the covalent binding.

Research Organization:
INSERM U 75, CHU Necker-Enfants Malades, Paris, France
OSTI ID:
5558487
Journal Information:
Toxicol. Appl. Pharmacol.; (United States), Journal Name: Toxicol. Appl. Pharmacol.; (United States) Vol. 77:1; ISSN TXAPA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANESTHETICS
ANIMALS
ANTICONVULSANTS
AZINES
BARBITURATES
BIOCHEMICAL REACTION KINETICS
BODY
CARBON 14 COMPOUNDS
CARBON COMPOUNDS
CARBON MONOXIDE
CARBON OXIDES
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM DEPRESSANTS
CHALCOGENIDES
CHEMICAL BONDS
COMPARATIVE EVALUATIONS
COVALENCE
DIGESTIVE SYSTEM
DRUGS
ENZYME INHIBITORS
ENZYMES
ESTERASES
GLANDS
HETEROCYCLIC COMPOUNDS
HOMOGENATES
HYDROLASES
HYPNOTICS AND SEDATIVES
IN VITRO
INSECTICIDES
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
LIVER
MAMMALS
METABOLISM
MICROSOMES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANIC OXYGEN COMPOUNDS
ORGANOIDS
ORGANS
OXIDES
OXYGEN COMPOUNDS
PESTICIDES
PHENOBARBITAL
PHOSPHORUS COMPOUNDS
PROTEINS
PYRIMIDINES
PYROPHOSPHATES
RATS
REACTION KINETICS
RESPONSE MODIFYING FACTORS
RODENTS
TRACER TECHNIQUES
VERTEBRATES