title: Roles of loop C and the loop B-C interval of the nicotinic receptor alpha subunit in its selective interactions with imidacloprid in insects.
abstract: To elucidate the mechanism of selective action of imidacloprid on insect nicotinic acetylcholine receptors (nAChRs), we examined the roles of loop C and the loop B-C interval region in receptor interactions with imidacloprid. The P242E mutation in loop C of the Drosophila SAD subunit (the second alpha-like Drosophila nicotinic acetylcholine receptor subunit, also called Dalpha2 subunit) reduced imidacloprid sensitivity of the SAD-chicken beta2 hybrid nAChR, whereas the E219P mutation of the alpha4 subunit increased the imidacloprid sensitivity of the alpha4beta2 nAChR. Deletion of the loop B-C interval region from the SAD subunit enhanced the effect of the P242E mutation on the SADbeta2 hybrid nAChR, suggesting important roles of the regions investigated in the nAChR-imidacloprid interactions.
authors.affiliation: Department of Agricultural Chemistry, Faculty of Agriculture, Kinki University, 3327-204 Nakamachi, Nara 631-8505, Japan.
authors.forename: Masaru
authors.initials: M
authors.lastname: Shimomura
authors.forename: Maiko
authors.initials: M
authors.lastname: Yokota
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Matsuda
authors.forename: David B
authors.initials: DB
authors.lastname: Sattelle
authors.forename: Koichiro
authors.initials: K
authors.lastname: Komai
mesh_terms: D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D002645:Chickens; D004305:Dose-Response Relationship, Drug; D004330:Drosophila; D007093:Imidazoles / Q000494:pharmacology*; D007313:Insecta / Q000187:drug effects*; D007306:Insecticides / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects; D016297:Mutagenesis, Site-Directed; D000073943:Neonicotinoids; D009574:Nitro Compounds; D009865:Oocytes; D018408:Patch-Clamp Techniques; D010944:Plants; D020836:Protein Structure, Quaternary; D021122:Protein Subunits / Q000737:chemistry / Q000378:metabolism*; D011978:Receptors, Nicotinic / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D011993:Recombinant Fusion Proteins / Q000378:metabolism; D016415:Sequence Alignment; D013329:Structure-Activity Relationship; D014162:Transfection; D014982:Xenopus laevis
chemical_list: D007093:Imidazoles; D007306:Insecticides; D000073943:Neonicotinoids; D009574:Nitro Compounds; D021122:Protein Subunits; D011978:Receptors, Nicotinic; D011993:Recombinant Fusion Proteins; C082359:imidacloprid; D000109:Acetylcholine