Ligands of the nicotinic acetylcholine receptor as insecticides (Extended summary)

Insect nicotinic acetyl receptors (nAChR) are targets of growing importance and, since the early 1990s, the number of such highly effective insecticides as imidacloprid and spinosyn has grown. Several natural compounds, e.g. dihydro-beta-erythroidine, methyl caconitine and paraherquamide, showing high affinity to the same receptor, were considerably less active as insecticides, most likely because of their antagonistic action. Our observations on aphids after ingestion of the antagonistic compound dihydro-beta-crythroidine revealed anti-feedant-like properties. As a consequence, the symptomology of poisoning was totally different between agonists and antagonists of the nAChR. Electrophysiological (whole-cell voltage clamp) measurements in isolated housefly neurones revealed that agonism seems to be a prerequisite for insecticidal activity. Furthermore, we were able to demonstrate theexistence of two different subtypes of the nAChR in isolated locust neurones with different pharmacology and ion-channel properties. [ABSTRACT FROM AUTHOR]