Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex

Kevin M. Crofton; Lawrence W. Reiter; Richard Mailman

doi:10.1016/0378-4274(87)90205-0

Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex

Kevin M. Crofton, Lawrence W. Reiter, Richard Mailman

Research output: Contribution to journal › Article › peer-review

24 Scopus citations

Abstract

Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on [³H]flunitrazepam (FLU), [³H]muscimol (MUS), and [³⁵S]t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with [³H]FLU and [³H]MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of [³⁵S]TBPS at concentrations as high as 50 μM. Type II pyrethroids inhibited [³⁵S]TBPS binding to rat brain synaptosomes with K_i, values ranging from 5-10 μM. The data presented here suggest that the interaction of Type II pyrethroids with the γ-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.

Original language	English (US)
Pages (from-to)	183-190
Number of pages	8
Journal	Toxicology Letters
Volume	35
Issue number	2-3
DOIs	https://doi.org/10.1016/0378-4274(87)90205-0
State	Published - Feb 1987

All Science Journal Classification (ASJC) codes

Toxicology

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10.1016/0378-4274(87)90205-0

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title = "Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex",

abstract = "Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on [3H]flunitrazepam (FLU), [3H]muscimol (MUS), and [35S]t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with [3H]FLU and [3H]MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of [35S]TBPS at concentrations as high as 50 μM. Type II pyrethroids inhibited [35S]TBPS binding to rat brain synaptosomes with Ki, values ranging from 5-10 μM. The data presented here suggest that the interaction of Type II pyrethroids with the γ-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.",

author = "Crofton, {Kevin M.} and Reiter, {Lawrence W.} and Richard Mailman",

note = "Funding Information: * This manuscript has been reviewed by the Health Effects Research Laboratory, U.S. Environmental Protection Agency, and approved for publication. Mention of trade names or commercial products does not constitute endorsement or r~ommendation for use. ** To whom correspondence and reprint requests should be mailed at address b.",

year = "1987",

month = feb,

doi = "10.1016/0378-4274(87)90205-0",

language = "English (US)",

volume = "35",

pages = "183--190",

journal = "Toxicology Letters",

issn = "0378-4274",

publisher = "Elsevier Ireland Ltd",

number = "2-3",

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T1 - Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex

AU - Crofton, Kevin M.

AU - Reiter, Lawrence W.

AU - Mailman, Richard

N1 - Funding Information: * This manuscript has been reviewed by the Health Effects Research Laboratory, U.S. Environmental Protection Agency, and approved for publication. Mention of trade names or commercial products does not constitute endorsement or r~ommendation for use. ** To whom correspondence and reprint requests should be mailed at address b.

PY - 1987/2

Y1 - 1987/2

N2 - Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on [3H]flunitrazepam (FLU), [3H]muscimol (MUS), and [35S]t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with [3H]FLU and [3H]MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of [35S]TBPS at concentrations as high as 50 μM. Type II pyrethroids inhibited [35S]TBPS binding to rat brain synaptosomes with Ki, values ranging from 5-10 μM. The data presented here suggest that the interaction of Type II pyrethroids with the γ-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.

AB - Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on [3H]flunitrazepam (FLU), [3H]muscimol (MUS), and [35S]t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with [3H]FLU and [3H]MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of [35S]TBPS at concentrations as high as 50 μM. Type II pyrethroids inhibited [35S]TBPS binding to rat brain synaptosomes with Ki, values ranging from 5-10 μM. The data presented here suggest that the interaction of Type II pyrethroids with the γ-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.

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JO - Toxicology Letters

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ER -

Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex

Abstract

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