Abstract

The interaction of several formamidine pesticides, chlordimeform (CDM), N-demethylchlordimeform (DCDM) and amitraz with octopamine receptor(s) and the resulting enhancement of cyclic-AMP (cAMP) production in vitro were investigated in the two-spotted spider mite, Tetranychus urticae Koch. DCDM and amitraz clearly stimulated the production of cAMP when added to a homogenate of the spider mite. Among various biogenic amines tested, octopamine and synephrine were most active but dopamine (DA) and 5-hydroxytroptamine showed only marginal potency to elevate cAMP production. An additivity study was devised to find whether these formamidines interact with the same target site as octopamine. The results indicate that all these chemicals act on the same receptor which functions to transduce the signal of certain biogenic amines to elevate the intracellular cAMP level. Phentolamine (PH) and propranolol (PR) showed an antagonistic effect against the portion of cAMP production which was elevated by DCDM. Among pesticides tested, deltamethrin, fenvalerate, DDT and benzenehexachloride showed no such effect, whereas dicofol, chlorobenzilate, parathion and aldicarb showed slight stimulatory effects on cAMP production. Both DCDM and octopamine cause an increase in the phosphorylation of proteins that are also phosphorylated by exogenous cAMP-dependent protein kinase. The results of pharmacological characterization studies confirmed the overall theory that the agonistic effects of formamidines are expressed primarily through the octopamine-sensitive adenylate cyclase.

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