Flupyrimin

Flupyrimin (FLP) is a novel insecticide with a trifluoroacetyl pharmacophore and an antagonist of insect nicotinic acetylcholine receptors (nAChRs)^{[1, 2]}. nAChRs are ligand-gated ion channels that are primarily expressed in the central nervous system of insects and are direct targets of insecticides^[3]. Flupyrimin is a novel nicotinoid insecticide with unique biological properties, no cross-resistance, and is safe for pollinating insects^[4]. Flupyrimin can quench the intrinsic fluorescence of human serum albumin/bovine serum albumin (HSA/BSA)^[5]. Flupyrimin shows good efficacy against rice pests that are insensitive to neonicotinoids^[6].

References:
[1] Umetsu N, Shirai Y. Development of novel pesticides in the 21st century[J]. Journal of Pesticide Science, 2020, 45(2): 54-74.
[2] Terajima T, Suzuki T, Horikoshi R, et al. Deciphering the flupyrimin binding surface on the insect nicotinic acetylcholine receptor[J]. Journal of Agricultural and Food Chemistry, 2021, 69(33): 9551-9556.
[3] Yuan X F, Zhong H, Xia Z Y, et al. Integrated transcriptome and 1H NMR-based metabolome to explore the potential mechanism of Spodoptera litura in response to flupyrimin[J]. Pesticide Biochemistry and Physiology, 2024, 205: 106146.
[4] Lu X, Xu H, Zhang X, et al. Design, synthesis and bioactivity of novel low bee-toxicity compounds based on flupyrimin[J]. Molecules, 2022, 27(18): 6133.
[5] Zhao Z, Shi T, Chu Y, et al. Comparison of the interactions of flupyrimin and nitenpyram with serum albumins via multiple analysis methods[J]. Chemosphere, 2022, 289: 133139.
[6] Jeschke P. Status and outlook for acaricide and insecticide discovery[J]. Pest management science, 2021, 77(1): 64-76.

Flupyrimin（FLP）是一种具有三氟乙酰基药效团的新型杀虫剂，是昆虫烟碱乙酰胆碱受体（nAChR）的拮抗剂^{[1, 2]}。nAChR是主要在昆虫中枢神经系统中表达的配体门控离子通道，是杀虫剂的直接靶标^[3]。Flupyrimin是一种新型烟碱类杀虫剂，具有独特的生物学特性，无交叉耐药性，对传粉昆虫安全^[4]。Flupyrimin可以猝灭人血清白蛋白/牛血清白蛋白（HSA/BSA）的内源荧光^[5]。Flupyrimin对新烟碱不敏感的水稻害虫表现出良好的效力^[6]。