期刊
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY
卷 41, 期 7, 页码 440-445出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.ibmb.2011.04.005
关键词
Nitroconjugated neonicotinoid; Nicotinic acetylcholine receptors; Nilaparvata lugens; Insecticidal activity; Y1515 mutation
资金
- National Basic Research Program of China (973 Program) [2010CB126100, 2010CB126200]
- National Science Foundation China [30971917]
- Foundation for the Author of National Excellent Doctoral Dissertation of PR China [2007860]
- National High Technology Research and Development Program of China (863 Program) [2010AA10A204]
- Shanghai Foundation of Science and Technology [09XD1401300]
Neonicotinoid insecticides, such as imidacloprid, are selective agonists of the insect nicotinic acetylcholine receptors (nAChRs) with -NO(2) or -CN group in trans-configuration. Previously we reported the excellent insecticidal activity of a series of nitroconjugated neonicotinoids with -NO(2) or -CN group in cis-configuration by replacing nitromethylene pharmacophore with a nitroconjugated system. To understand the action mode of these nitroconjugated neonicotinoids, a representative member IPPA152201 was chosen to perform toxicity and pharmacology studies. IPPA152201 showed a comparable toxicity with imidacloprid against Nilaparvata lugens in a susceptible strain and had no significant cross-resistance in an imidacloprid resistant strain. IPPA152201 showed good efficacies on the isolated cockroach neurons (pEC(50) = 5.91 +/- 0.14) and the evoked responses by IPPA152201 could be blocked by the typical nAChRs antagonists methyllycaconitine citrate (MLA) and dihydro-beta-erythroidine (DH beta E), with pIC(50) of 6.56 +/- 0.07 and 6.89 +/- 0.12. The efficacy of IPPA152201 on hybrid receptors NI alpha 1/beta 2 in Xenopus oocytes and response inhibition by MLA and DH beta E were also observed. These data demonstrate that IPPA152201 acts on insect nAChRs as an agonist. In addition, the influence of a NI alpha 1 mutation (Y151S), which has been linked to the lab-generated neonicotinoid resistance in N. lugens, has been examined. Compared to the wildtype NI alpha 1/beta 2, this mutation reduced I(max) for IPPA152201 to 63.2% and caused a 1.5-fold increase in EC(50), which is much smaller than the effects on imidacloprid. The high insecticidal activity and little influence by Y151S mutation make IPPA152201 to be a potential insecticide to manage N. lugens. (C) 2011 Elsevier Ltd. All rights reserved.
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