In vivo and in vitro experiments were used to study the effects of formamidines in the locust, Locusta migratoria migratorioides. In vivo the lethal and the antifeeding effects, in vitro the inhibition of the binding of a selective 3H-ligand to the receptors of octopamine, tyramine, dopamine, serotonin and γ-amino butiric acid were studied. We have demonstrated that demethylchlordimeform is specific agonist to octopamine receptor, having high affinity to octopamine receptor, a moderate affinity to tyramine receptor and a low affinity to dopamine, serotonin and to γ-amino butiric acid receptors. The demethylated chlordimeform analogoues, demethylchlordimeform and didemethylchlordimeform have higher affinity to the octopamine receptor than the parent compound. The formamidines had a toxic and an antifeeding effects when injected into the locust. The half lethal doses (LD50) and the feeding inhibition were correlated with the affinity of the compounds (K(i)). The ring substitutions of the molecule have alterated the both affinity and in vivo effect of the compounds. The most effective ring substitution pattern is 2,4-disubstitution with a combination of methyl groups or halogens. Our results suggest that the lethal effect of formamidines is mediated through the octopamine receptor.
|Number of pages||7|
|Journal||Acta biologica Hungarica|
|Publication status||Published - Nov 10 1999|
- Insect Locusta migratoria migratorioides
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Environmental Science(all)