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Title: Interactions of pyrethroid insecticides with GABA sub A and peripheral-type benzodiazepine receptors

Abstract

Pyrethroid insecticides are potent proconvulsants in the rat. All pyrethroids evincing proconvulsant activity elicited a similar 25-30% maximal reduction of seizure threshold. The Type II pyrethroids were the most potent proconvulsants with 1R{alpha}S, cis cypermethrin having an ED{sub 50} value of 6.3 nmol/kg. The proconvulsant activity of both Type I and Type II pyrenthroids was blocked by pretreatment with PK 11195, the peripheral-type benzodiazepine receptor (PTBR) antagonist. In contrast, phenytoin did not antagonize the proconvulsant activity of either deltamethrin or permethrin. Pyrethroids displaced the specific binding of ({sup 3}H)Ro5-4864 to rat brain membranes with a significant correlation between the log EC{sub 50} values for their activities as proconvulsants and the log IC{sub 50} values for their inhibition of ({sup 3}H)Ro5-4864 binding. Both Ro5-4864 and pyrethroid insecticides were found to influence specific ({sup 35}S)TBPS binding in a GABA-dependent manner. PK 11195 and the Type II pyrethroid, deltamethrin antagonized the Ro5-4864-induced modulation of ({sup 35}S)TBPS binding. Pyrethroid insecticides, Ro5-4864 and veratridine influenced GABA-gated {sup 36}Chloride influx. Moreover, the Type II pyrethroids elicited an increase in {sup 36}chloride influx in the absence of GABA-stimulation. Both of these actions were antagonized by PK 11195 and tetrodotoxin.

Authors:
Publication Date:
Research Org.:
Oregon State Univ., Corvallis, OR (USA)
OSTI Identifier:
6940398
Resource Type:
Miscellaneous
Resource Relation:
Other Information: Thesis (Ph. D.)
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; AMINOBUTYRIC ACID; RECEPTORS; INSECTICIDES; BIOCHEMICAL REACTION KINETICS; BRAIN; CELL MEMBRANES; CHLORINE 36; RATS; SULFUR 35; TRACER TECHNIQUES; TRITIUM COMPOUNDS; AMINO ACIDS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BODY; CARBOXYLIC ACIDS; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; CHLORINE ISOTOPES; DAYS LIVING RADIOISOTOPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; EVEN-ODD NUCLEI; HYDROGEN COMPOUNDS; ISOTOPE APPLICATIONS; ISOTOPES; KINETICS; LIGHT NUCLEI; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-ODD NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANS; PESTICIDES; PROTEINS; RADIOISOTOPES; REACTION KINETICS; RODENTS; SULFUR ISOTOPES; VERTEBRATES; YEARS LIVING RADIOISOTOPES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Devaud, L L. Interactions of pyrethroid insecticides with GABA sub A and peripheral-type benzodiazepine receptors. United States: N. p., 1988. Web.
Devaud, L L. Interactions of pyrethroid insecticides with GABA sub A and peripheral-type benzodiazepine receptors. United States.
Devaud, L L. 1988. "Interactions of pyrethroid insecticides with GABA sub A and peripheral-type benzodiazepine receptors". United States.
@article{osti_6940398,
title = {Interactions of pyrethroid insecticides with GABA sub A and peripheral-type benzodiazepine receptors},
author = {Devaud, L L},
abstractNote = {Pyrethroid insecticides are potent proconvulsants in the rat. All pyrethroids evincing proconvulsant activity elicited a similar 25-30% maximal reduction of seizure threshold. The Type II pyrethroids were the most potent proconvulsants with 1R{alpha}S, cis cypermethrin having an ED{sub 50} value of 6.3 nmol/kg. The proconvulsant activity of both Type I and Type II pyrenthroids was blocked by pretreatment with PK 11195, the peripheral-type benzodiazepine receptor (PTBR) antagonist. In contrast, phenytoin did not antagonize the proconvulsant activity of either deltamethrin or permethrin. Pyrethroids displaced the specific binding of ({sup 3}H)Ro5-4864 to rat brain membranes with a significant correlation between the log EC{sub 50} values for their activities as proconvulsants and the log IC{sub 50} values for their inhibition of ({sup 3}H)Ro5-4864 binding. Both Ro5-4864 and pyrethroid insecticides were found to influence specific ({sup 35}S)TBPS binding in a GABA-dependent manner. PK 11195 and the Type II pyrethroid, deltamethrin antagonized the Ro5-4864-induced modulation of ({sup 35}S)TBPS binding. Pyrethroid insecticides, Ro5-4864 and veratridine influenced GABA-gated {sup 36}Chloride influx. Moreover, the Type II pyrethroids elicited an increase in {sup 36}chloride influx in the absence of GABA-stimulation. Both of these actions were antagonized by PK 11195 and tetrodotoxin.},
doi = {},
url = {https://www.osti.gov/biblio/6940398}, journal = {},
number = ,
volume = ,
place = {United States},
year = {Fri Jan 01 00:00:00 EST 1988},
month = {Fri Jan 01 00:00:00 EST 1988}
}

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