Abstract
The acute administration of 1R,cis,αS-cypermethrin, deltamethrin fenvalerate and permethrin produced a dose-dependent lowering of the dose of pentylenetetrazol required to elicit a seizure in rats. The proconvulsant action of cypermethrin displayed stereospecificity in that the 1R,cis,αS isomer of cypermethrin was the most potent compound tested, while the non-insecticidal isomer, 1S,cis,αR-cypermethrin, was devoid of proconvulsant activity. Pretreatment of rats with PK 11195, an antagonist of the peripheral-type benzodiazepine binding site, elicited a complete reversal of the proconvulsant actions of both deltamethrin and permethrin. In contrast, pretreatment with phenytoin did not alter the pyrethroid-induced proconvulsant activity. These results suggest that the effect of pyrethroids on pentylenetetrazol seizure threshold are mediated via an interaction with peripheral-type benzodiazepine binding sites.
| Original language | English |
|---|---|
| Pages (from-to) | 269-273 |
| Number of pages | 5 |
| Journal | European Journal of Pharmacology |
| Volume | 121 |
| Issue number | 2 |
| DOIs | |
| State | Published - Feb 18 1986 |
| Externally published | Yes |
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All Science Journal Classification (ASJC) codes
- Cellular and Molecular Neuroscience
- Pharmacology
Cite this
PK 11195 antagonism of pyrethroid-induced proconvulsant activity. / Devaud, Leslie L.; Szot, Patricia; Murray, Thomas F.
In: European Journal of Pharmacology, Vol. 121, No. 2, 18.02.1986, p. 269-273.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - PK 11195 antagonism of pyrethroid-induced proconvulsant activity
AU - Devaud, Leslie L.
AU - Szot, Patricia
AU - Murray, Thomas F.
PY - 1986/2/18
Y1 - 1986/2/18
N2 - The acute administration of 1R,cis,αS-cypermethrin, deltamethrin fenvalerate and permethrin produced a dose-dependent lowering of the dose of pentylenetetrazol required to elicit a seizure in rats. The proconvulsant action of cypermethrin displayed stereospecificity in that the 1R,cis,αS isomer of cypermethrin was the most potent compound tested, while the non-insecticidal isomer, 1S,cis,αR-cypermethrin, was devoid of proconvulsant activity. Pretreatment of rats with PK 11195, an antagonist of the peripheral-type benzodiazepine binding site, elicited a complete reversal of the proconvulsant actions of both deltamethrin and permethrin. In contrast, pretreatment with phenytoin did not alter the pyrethroid-induced proconvulsant activity. These results suggest that the effect of pyrethroids on pentylenetetrazol seizure threshold are mediated via an interaction with peripheral-type benzodiazepine binding sites.
AB - The acute administration of 1R,cis,αS-cypermethrin, deltamethrin fenvalerate and permethrin produced a dose-dependent lowering of the dose of pentylenetetrazol required to elicit a seizure in rats. The proconvulsant action of cypermethrin displayed stereospecificity in that the 1R,cis,αS isomer of cypermethrin was the most potent compound tested, while the non-insecticidal isomer, 1S,cis,αR-cypermethrin, was devoid of proconvulsant activity. Pretreatment of rats with PK 11195, an antagonist of the peripheral-type benzodiazepine binding site, elicited a complete reversal of the proconvulsant actions of both deltamethrin and permethrin. In contrast, pretreatment with phenytoin did not alter the pyrethroid-induced proconvulsant activity. These results suggest that the effect of pyrethroids on pentylenetetrazol seizure threshold are mediated via an interaction with peripheral-type benzodiazepine binding sites.
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U2 - 10.1016/0014-2999(86)90499-1
DO - 10.1016/0014-2999(86)90499-1
M3 - Article
VL - 121
SP - 269
EP - 273
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 2
ER -