Diverse actions of neonicotinoids on chicken α7, α4β2 and Drosophila-chicken SADβ2 and ALSβ2 hybrid nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes

Makoto Ihara, Kazuhiko Matsuda, Maiko Otake, Morihiko Kuwamura, Masaru Shimomura, Koichiro Komai, Miki Akamatsu, Valérie Raymond, David B. Sattelle

    Research output: Contribution to journalArticlepeer-review

    Abstract

    The 2-nitroimino-imidazolidine and related moieties are structural features of neonicotinoid insecticides acting on nicotinic acetylcholine receptors (nicotinic AChRs). To evaluate these moieties in neonicotinoid interactions with nicotinic AChR α subunits, the actions of imidacloprid and related compounds on the chicken α7, α4β2 and Drosophila melanogaster-chicken hybrid (SADβ2 and ALSβ2) receptors expressed in Xenopus laevis oocytes were studied by voltage-clamp electrophysiology. Imidacloprid and nitenpyram were partial agonists and a nitromethylene analog of imidacloprid (CH-IMI) was a full agonist of the α7 receptor, whereas their agonist actions on the α4β2 receptor were very weak, contrasting with full agonist actions of DN-IMI, a desnitro derivative of imidacloprid. The neonicotinoids and DN-IMI were either full or partial agonists of the SADβ2 receptors. Nitenpyram and DN-IMI were partial agonists of the ALSβ2 receptor, whereas imidacloprid and CH-IMI scarcely activated the ALSβ2 receptor. Imidacloprid and CH-IMI in fact suppressed ACh-induced responses of the ALSβ2 receptor, whereas imidacloprid potentiated and CH-IMI suppressed ACh-induced responses of the α4β2 receptor. These results suggest that interactions with α subunits of the 2-nitroimino-imidazolidine moiety of imidacloprid play a role in determining not only agonist and antagonist actions on all four receptors, but also the potentiation of ACh-induced responses of the α4β2 receptor. © 2003 Elsevier Science Ltd. All rights reserved.
    Original languageEnglish
    Pages (from-to)133-144
    Number of pages11
    JournalNeuropharmacology
    Volume45
    Issue number1
    DOIs
    Publication statusPublished - Jul 2003

    Keywords

    • Chicken α4β2 nicotinic receptor
    • Chicken α7 nicotinic receptor
    • Drosophila ALS chicken β2 hybrid nicotinic receptor
    • Drosophila SAD chicken β2 hybrid nicotinic receptor
    • Neonicotinoids
    • Nicotinic acetylcholine receptor

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