XB-ART-53957Br J Pharmacol. August 29, 2017;
Neonicotinoid insecticides differently modulate acetycholine-induced currents on mammalian α7 nicotinic acetylcholine receptor.
Neonicotinoid insecticides are described as poor agonists of mammalian nicotinic acetylcholine receptors. In this paper, we provide evidence that they diffenrently act on mammalian nicotinic receptors. Two-electrode voltage-clamp electrophysiology was used to characterized the pharmacology of neonicotinoid insecticides on α7 receptors expressed in Xenopus oocytes. Single and combined application of clothianidin, acetamiprid and thiamethoxam were tested. The neonicotinoid insecticides, clothianidin and acetamiprid were partial agonists of mammalian neuronal α7 nicotinic receptors and thiamethoxam, a neonicotinoid insecticide, which is converted to clothianidin in insect and plant tissues had no effect. Pretreatment of 10 μM clothianidin and acetamiprid with 100 μM acetylcholine, significantly enhanced the subsequent acetylcholine-evoked currents whereas, 10 μM thiamethoxam reduced acetylcholine-induced current amplitudes. Moreover, the combinations of the three neonicotinoids decreased the ACh evoked currents. The present findings suggest that neonicotinoid insecticides differently affect α7 nicotinic acetylcholine receptors and can modulate acetylcholine-induced current. In final, the data indicate a previous unknown modulation of mammalian α7 receptors by combined application of clothianidin, acetamiprid and thiamethoxam.
PubMed ID: 28853147
Article link: Br J Pharmacol.