Abstract
An ester of the acid moiety of kadethrin, one of pyrethroid insecticides, with a photoreactive alcohol containing a diazirine group was synthesized as a probe for elucidating the target site of pyrethroids. Its insecticidal potency against American cockroaches agreed well with the value predicted from a correlation equation that was previously established by quantitative structure-activity analysis for a set of esters of the acid with meta-substituted benzyl alcohols. The compound modified the membrane potentials of crayfish and cockroach giant axons, inducing depolarizing afterpotentials as well as depolarizing the resting membranes. The inward sodium currents in the crayfish giant axon and rat pituitary tumor cells, GH3, were also modified by the compound. Decay of the current was slowed to induce a residual current, associated with enhancement and prolongation of the tail current.
