Abstract
The functional expression of the cockroach Pameα7 nicotinic acetylcholine receptor subunit has been previously studied, and was found to be able to form a homomeric receptor when expressed in Xenopus laevis oocytes. In this study, we found that the neonicotinoid insecticide imidacloprid is unable to activate the cockroach Pameα7 receptor, although thiacloprid induces low inward currents, suggesting that it is a partial agonist. In addition, the co-application or 5 min pretreatment with 10 µM imidacloprid increased nicotine current amplitudes, while the co-application or 5 min pretreatment with 10 µM thiacloprid decreased nicotine-evoked current amplitudes by 54% and 28%, respectively. This suggesting that these two representatives of neonicotinoid insecticides bind differently to the cockroach Pameα7 receptor. Interestingly, the docking models demonstrate that the orientation and interactions of the two insecticides in the cockroach Pameα7 nAChR binding pocket are very similar. Electrophysiological results have provided evidence to suggest that imidacloprid and thiacloprid could act as modulators of the cockroach Pameα7 receptors.
Highlights
Nicotinic acetylcholine receptors are representative members of the Cysloop ligand-gated ion channels (LGICs) superfamily, alongside GABA, glycine, and 5-HT3 receptors [1,2,3]
Insecticides on Nicotine-Induced roach Nicotinic acetylcholine receptors (nAChRs), we have studied theCurrents effect of neonicotinoid insecticid previously demonstrated to that system expressed theyWe have been understood becockroach agonistsnervous of cockroach nAChRshomomeric
No of macroscopic roach Pameα7 nAChRs, we have studied the effect of neonicotinoid insecticides, since they were detected within the recorded limits of detection (Figure 2)
Summary
Nicotinic acetylcholine receptors (nAChRs) are representative members of the Cysloop ligand-gated ion channels (LGICs) superfamily, alongside GABA, glycine, and 5-HT3 receptors [1,2,3]. LGICs, with the five subunits being symmetrically or pseudosymmetrically arranged around a central ion-conducting pore, from homo- or heteropentamers of the related subunits [1,2,3] These properties have made nAChRs important targets for human and veterinary drugs, as well as insecticides. Two α-Bgt-insensitive receptors were identified as nAChR1, which are sensitive to IMI and selectively blocked by d-tubocurarine (d-TC), while nAChR2 is inhibited by mecamylamine [13,15,16,17] Together, these studies have been used to monitor and analyze the mode of action of neonicotinoid insecticides on insect nAChRs, in order to understand the mechanisms of resistance
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