Two types of cage convulsant action at the GABA-gated chloride channel.
Cage convulsants appear to fall into two groups based on correlations between their potency for inhibiting [35S]t-butylbicyclophosphorothionate binding or gamma-aminobutyric acid-stimulated 36chloride uptake in brain membrane preparations and their toxicity to mice. Polychlorocycloalkanes, picrotoxinin and 2,6,7-trioxabicyclo[2.2.2]octanes with large 1-substituents exhibit high potency in these in vitro brain membrane systems relative to their toxicity (type A action). In contrast, trioxabicyclooctanes with small 1-substituents and tetramethylenedisulfotetramine show much lower in vitro potency relative to their toxicity (type B action). Compounds with type A action are generally more potent insecticides than those with type b action.
Palmer
C J
CJ
Department of Entomological Sciences, University of California, Berkeley 94720.
Casida
J E
JE
D000818:Animals; D001665:Binding Sites; D002540:Cerebral Cortex / Q000378:metabolism; D002712:Chlorides / Q000378:metabolism*; D003292:Convulsants / Q000145:classification / Q000494:pharmacology*; D006801:Humans; D007306:Insecticides / Q000145:classification; D007473:Ion Channels / Q000187:drug effects*; D051379:Mice; D005680:gamma-Aminobutyric Acid / Q000502:physiology*
D002712:Chlorides; D003292:Convulsants; D007306:Insecticides; D007473:Ion Channels; D005680:gamma-Aminobutyric Acid