Correlations of the electrophysiological activity of neonicotinoids with their binding and insecticidal activities
- 12 June 2003
- journal article
- research article
- Published by Wiley in Pest Management Science
- Vol. 59 (9) , 1023-1030
- https://doi.org/10.1002/ps.729
Abstract
The electrophysiological actions of various neonicotinoids, including substituted benzyl derivatives, against recombinant Drosophila SAD/chicken β2 hybrid nicotinic acetylcholine receptor (nAChR) were measured to analyze the relationships between the in vivo (insecticidal) and in vitro (binding and agonist) activities. Most of the neonicotinoids tested were capable of inducing inward currents by activating the hybrid nAChRs expressed in Xenopus laevis oocytes, whereas some compounds had no agonist activity and only blocked the acetylcholine-induced currents. Variations in the agonist activity were well correlated with those in the binding potency evaluated using [3H]imidacloprid as well as insecticidal activities. Copyright © 2003 Society of Chemical IndustryKeywords
This publication has 30 references indexed in Scilit:
- Nicotinic acetylcholine receptor binding of imidacloprid‐related diaza compounds with various ring sizes and their insecticidal activity against Musca domesticaPest Management Science, 2002
- Interaction of dinotefuran and its analogues with nicotinic acetylcholine receptors of cockroach nerve cordsPest Management Science, 2001
- Chemistry and biology of thiamethoxam: a second generation neonicotinoidPest Management Science, 2001
- Insecticidal and binding activities of N3‐substituted imidacloprid derivatives against the housefly Musca domestica and the α‐bungarotoxin binding sites of nicotinic acetylcholine receptorsPest Management Science, 2001
- Prediction of the binding mode of imidacloprid and related compounds to house-fly head acetylcholine receptors using three-dimensional QSAR analysisPesticide Science, 1998
- Effects of the α subunit on imidacloprid sensitivity of recombinant nicotinic acetylcholine receptorsBritish Journal of Pharmacology, 1998
- Topology of ligand binding sites on the nicotinic acetylcholine receptorBrain Research Reviews, 1997
- Molecular Mechanism for Selective Toxicity of Nicotinoids and NeonicotinoidsJournal of Pesticide Science, 1995
- Binding of Nicotinoids and the Related Compounds to the Insect Nicotinic Acetyicholine ReceptorJournal of Pesticide Science, 1992
- Sensitive nicotinic and mixed nicotinic-muscarinic receptors in insect neurosecretory cellsBrain Research, 1990