Fluxametamide is an antagonist of GABA- and Glu-gated chloride channels (GABACls and GluCls) with IC50 value of 1.95nM and 225nM, respectively[1]. Fluxametamide mainly bound in transmembrane domain (TM)3 domain by forming amide-pi stacked with Gly316, pi-alkyl with Val313, Leu315 and Phe319 [2]. Fluxametamide has been widely used as an insecticide, inhibiting the growth of various pests, including Lepidoptera, Acarina, Thysanoptera, and Diptera[3].
In vivo, Fluxametamide (dissolved in the water environment) has a relatively high toxicity to zebrafish with LC50=0.785mg/L after a 96-hour treatment[4].
References:
[1] Asahi M, Kobayashi M, Kagami T, et al. Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels[J]. Pesticide biochemistry and physiology, 2018, 151: 67-72.
[2] Yin X, Li S, Tian Q, et al. Comparison of the toxicity and pharmacological effects of two insecticides against the Asian corn borer, Ostrinia furnacalis[J]. Pesticide Biochemistry and Physiology, 2025: 106597.
[3] Li R, Pan X, Wang Q, et al. Development of S-fluxametamide for bioactivity improvement and risk reduction: systemic evaluation of the novel insecticide fluxametamide at the enantiomeric level[J]. Environmental science & technology, 2019, 53(23): 13657-13665.
[4] Huang Q, Jia Z, Wu S, et al. The acute toxicity, mechanism, bioconcentration and elimination of fluxametamide on zebrafish (Danio rerio)[J]. Environmental Pollution, 2023, 317: 120808.
Fluxametamide是一种GABA和谷氨酸门控氯离子通道的拮抗剂，对GABACls和GluCls的IC50值分别为1.95nM和225nM[1]。Fluxametamide主要通过在跨膜域（TM3）中与Gly316形成酰胺-π堆积以及与Val313、Leu315和Phe319形成π-烷基堆积的方式进行结合[2]。Fluxametamide已作为杀虫剂广泛应用，可抑制包括鳞翅目、螨类、缨翅目和双翅目在内的多种害虫的生长[3]。
在体内，将Fluxametamide溶解于水环境中处理斑马鱼96小时，表现出相对较高的毒性，LC50值为0.785mg/L[4]。