Action of insecticidal N-alkylamides at site 2 of the voltage-sensitive sodium channel
- Cornell Univ., Geneva, NY (USA)
Nine synthetic N-alkylamides were examined as inhibitors of the specific binding of ({sup 3}H)batrachotoxinin A 20{alpha}-benzoate (({sup 3}H)BTX-B) to sodium channels and as activators of sodium uptake in mouse brain synaptoneurosomes. In the presence of scorpion (Leiurus quinquestriatus) venom, the six insecticidal analogues were active as both inhibitors of ({sup 3}H)BTX-B binding and stimulators of sodium uptake. These findings are consistent with an action of these compounds at the alkaloid activator recognition site (site 2) of the voltage-sensitive sodium channel. The three noninsecticidal N-alkylamides also inhibited ({sup 3}H)BTX-B binding but were ineffective as activators of sodium uptake. Concentration-response studies revealed that some of the insecticidal amides also enhanced sodium uptake through a second, high-affinity interaction that does not involve site 2, but this secondary effect does not appear to be correlated with insecticidal activity. The activities of N-alkylamides as sodium channel activators were influenced by the length of the alkenyl chain and the location of unsaturation within the molecule. These results further define the actions of N-alkylamides on sodium channels and illustrate the significance of the multiple binding domains of the sodium channel as target sites for insect control agents.
- OSTI ID:
- 5941448
- Journal Information:
- Journal of Agricultural and Food Chemistry; (USA), Vol. 38:8; ISSN 0021-8561
- Country of Publication:
- United States
- Language:
- English
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INSECTICIDES
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ELECTROPHYSIOLOGY
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STRUCTURE-ACTIVITY RELATIONSHIPS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UPTAKE
ALKALI METALS
ANIMALS
BODY
CENTRAL NERVOUS SYSTEM
CHANNELING
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ISOTOPE APPLICATIONS
KINETICS
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551001* - Physiological Systems- Tracer Techniques