Roles of loop C and the loop B-C interval of the nicotinic receptor alpha subunit in its selective interactions with imidacloprid in insects.
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.
Shimomura
Masaru
M
Department of Agricultural Chemistry, Faculty of Agriculture, Kinki University, 3327-204 Nakamachi, Nara 631-8505, Japan.
Yokota
Maiko
M
Matsuda
Kazuhiko
K
Sattelle
David B
DB
Komai
Koichiro
K
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
D007093:Imidazoles; D007306:Insecticides; D000073943:Neonicotinoids; D009574:Nitro Compounds; D021122:Protein Subunits; D011978:Receptors, Nicotinic; D011993:Recombinant Fusion Proteins; C082359:imidacloprid; D000109:Acetylcholine