Mode of action of triflumezopyrim: A novel mesoionic insecticide which inhibits the nicotinic acetylcholine receptor

被引:98
作者
Cordova, Daniel [1 ]
Benner, Eric A. [1 ]
Schroeder, Mark E. [2 ]
Holyoke, Caleb W., Jr. [1 ]
Zhang, Wenming [1 ]
Pahutski, Thomas F. [1 ]
Leighty, Robert M. [1 ]
Vincent, Daniel R. [1 ]
Hamm, Jason C. [1 ]
机构
[1] DuPont Crop Protect, Stine Haskell Res Ctr, 1090 Elkton Rd, Newark, DE 19714 USA
[2] POB 184, Landenberg, PA 19350 USA
关键词
Nicotinic acetylcholine receptor; Mesoionic; Inhibitor; Antagonist; Desensitization; Periplaneta americana; Nilaparvata lugens; Myzus persicae; XENOPUS-LAEVIS OOCYTES; COCKROACH NEURONS; PERIPLANETA-AMERICANA; NILAPARVATA-LUGENS; ALPHA-BUNGAROTOXIN; BROWN PLANTHOPPER; AGONIST ACTIONS; NEONICOTINOIDS; RESISTANCE; BINDING;
D O I
10.1016/j.ibmb.2016.04.008
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Triflumezopyrim, a newly commercialized molecule from DuPont Crop Protection, belongs to the novel class of mesoionic insecticides. This study characterizes the biochemical and physiological action of this novel insecticide. Using membranes from the aphid, Myzus persicae, triflumezopyrim was found to displace H-3-imidacloprid with a K-i value of 43 nM with competitive binding results indicating that triflumezopyrim binds to the orthosteric site of the nicotinic acetylcholine receptor (nAChR). In voltage clamp studies using dissociated Periplaneta americana neurons, triflumezopyrim inhibits nAChR currents with an IC50 of 0.6 nM. Activation of nAChR currents was minimal and required concentrations >= 100 mu M. Xenopus oocytes expressing chimeric nAChRs (Drosophila alpha 2/chick beta 2) showed similar inhibitory effects from triflumezopyrim. In P. americana neurons, co-application experiments with acetylcholine reveal the inhibitory action of triflumezopyrim to be rapid and prolonged in nature. Such physiological action is distinct from other insecticides in IRAC Group 4 in which the toxicological mode of action is attributed to nAChR agonism. Mesoionic insecticides act via inhibition of the orthosteric binding site of the nAChR despite previous beliefs that such action would translate to poor insect control. Triflumezopyrim is the first commercialized insecticide from this class and provides outstanding control of hoppers, including the brown planthopper, Nilaparvata lugens, which is already displaying strong resistance to neonicotinoids such as imidacloprid. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:32 / 41
页数:10
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