Abstract:
:Pyrethroid insecticides are synthetic neurotoxins patterned after the naturally occurring pyrethrins. Their mechanism of action is thought to involve effects primarily at the voltage-sensitive sodium channel of both insect and mammalian neurons, although recent studies have raised the possibility that these compounds may also act at the gamma-aminobutyric acid receptor-chloride ionophore complex. Here we show that active pyrethroids of the alpha-cyano-3-phenoxybenzyl class allosterically enhance the binding of [3H]batrachotoxinin-A 20-alpha-benzoate to voltage-sensitive sodium channels of rat brain in a dose-dependent and stereospecific manner. Comparison of the rank order of potency for enhancement of [3H]batrachotoxinin-A 20-alpha-benzoate binding and insecticidal activity in a series of toxic stereoisomers of cypermethrin, representative of the class, reveals a correlation between the two measures. These results support a sodium channel site model for pyrethroid action and suggest a useful and practical method to help evaluate the relationship between effects at the sodium channel and insecticidal potency for members of this class of compounds.
journal_name
Mol Pharmacoljournal_title
Molecular pharmacologyauthors
Brown GB,Gaupp JE,Olsen RWsubject
Has Abstractpub_date
1988-07-01 00:00:00pages
54-9issue
1eissn
0026-895Xissn
1521-0111journal_volume
34pub_type
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journal_title:Molecular pharmacology
pub_type: 杂志文章
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journal_title:Molecular pharmacology
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journal_title:Molecular pharmacology
pub_type: 杂志文章
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journal_title:Molecular pharmacology
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更新日期:1994-08-01 00:00:00
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pub_type: 杂志文章
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pub_type: 杂志文章
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journal_title:Molecular pharmacology
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journal_title:Molecular pharmacology
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更新日期:1988-09-01 00:00:00
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journal_title:Molecular pharmacology
pub_type: 杂志文章
doi:
更新日期:1988-03-01 00:00:00
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journal_title:Molecular pharmacology
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更新日期:1984-09-01 00:00:00
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更新日期:1995-05-01 00:00:00
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更新日期:2021-02-01 00:00:00