Bifenthrin是一种拟除虫菊酯杀虫剂,其神经毒性作用的主要靶点是神经细胞膜的电压门控Na+通道。
Cas No.:82657-04-3
Sample solution is provided at 25 µL, 10mM.
Bifenthrin is a pyrethroid insecticide whose principal target of the neurotoxic action is the neuronal membrane’s voltage-gated Na+ channel [1]. Bifenthrin has greater photostability and insecticidal activity, but is neurotoxic to various animals, and its clinical signs of toxicity including tremors and convulsions. [1, 2].
Bifenthrin (20μM; 24h) induced a marked increase in PGE2, NO and TNF-alpha production in primary microglia; Bifenthrin (20μM; 24h) increased the expression of IL-6 and TNF-alpha mRNA in primary microglia [3]. Bifenthrin (1, 1.5μM; 24h) significantly decreased glutathione peroxidase activity in erythrocytes; Bifenthrin (1.5μM; 24h) induced hemolysis in erythrocytes [2].
Bifenthrin (30, 60ng/L; 14d) increased the number of congested blood vessels of juvenile rainbow trout [4]. Bifenthrin (8mg/kg; 7d; i.p.) induced local nuclear pyknosis and vacuolar degeneration of liver tissues in some BALB/c mouse specimens; Bifenthrin (2, 4, 8mg/kg; 7d; i.p.) resulted in a concentration-dependent increase in mitochondrial ROS generation of BALB/c mice [5]. Bifenthrin (0.6mg/kg; 6weeks; qod.; i.g.) significantly increased body weight of C57BL/6 mice; Bifenthrin (0.6mg/kg; 6weeks; qod.; i.g.) significantly downregulated the expression of HSL and ATGL while significantly upregulated the expression of LPL of C57BL/6 mice [6].
References:
[1] Moreira C V L, Ogbu J s, Monteiro K L C, et al. Bifenthrin under scrutiny: revisiting toxicological evidence amid regulatory gaps [J]. Journal of applied toxicology : JAT, 2026, 46(1): 61-77.
[2] Mukhtar F, Jilani K, Bibi I, et al. Stimulation of erythrocyte membrane blebbing by Bifenthrin induced oxidative stress [J]. Dose-response : a publication of International Hormesis Society, 2022, 20(1): 15593258221076710.
[3] Gargouri B, Yousif N M, Bouchard M, et al. Inflammatory and cytotoxic effects of bifenthrin in primary microglia and organotypic hippocampal slice cultures [J]. Journal of neuroinflammation, 2018, 15(1): 159.
[4] Magnuson J T, Caceres L, Sy N, et al. The use of non-targeted lipidomics and histopathology to characterize the neurotoxicity of Bifenthrin to juvenile rainbow trout (Oncorhynchus mykiss) [J]. Environmental science & technology, 2022, 56(16): 11482-11492.
[5] Zhang Y, Lu M, Zhou P, et al. Multilevel evaluations of potential liver injury of bifenthrin [J]. Pesticide biochemistry and physiology, 2015, 122: 29-37.
[6] Wei C, Wang X, Yao X, et al. Bifenthrin induces fat deposition by improving fatty acid uptake and inhibiting lipolysis in mice [J]. Journal of agricultural and food chemistry, 2019, 67(51): 14048-14055.
Bifenthrin是一种拟除虫菊酯杀虫剂,其神经毒性作用的主要靶点是神经细胞膜的电压门控Na+通道[1]。Bifenthrin具有较强的光稳定性和杀虫活性,但对多种动物具有神经毒性,其临床毒性表现为震颤和抽搐[1, 2]。
Bifenthrin(20μM;24h)显著促进原代小胶质细胞产生PGE2、NO和TNF-alpha;Bifenthrin(20μM;24h)提高原代小胶质细胞中IL-6和TNF-alpha的mRNA的表达水平[3]。Bifenthrin(1、1.5μM;24h)显著降低红细胞中的谷胱甘肽过氧化物酶活性;Bifenthrin(1.5μM;24h)引起红细胞溶血[2]。
Bifenthrin(30、60ng/L;14d)增加幼年彩虹鳟鱼的充血血管数量[4]。Bifenthrin(8mg/kg;7d;i.p.)会导致部分BALB/c小鼠样本的肺部组织出现局部核固缩和空泡变性;Bifenthrin(2、4、8mg/kg;7d;i.p.)导致BALB/c小鼠的线粒体ROS的生成呈现浓度依赖性增加[5]。Bifenthrin(0.6mg/kg;6weeks;qod.;i.g.)显著增加C57BL/6小鼠的体重;Bifenthrin(0.6mg/kg;6weeks;qod.;i.g.)显著下调C57BL/6小鼠HSL和ATGL的表达水平,上调LPL的表达水平[6]。
| Cell experiment [1]: | |
Cell lines | Primary microglia of Sprague Dawley rats |
Preparation Method | Microglial cells were exposed to Bifenthrin (DMSO as a control) for 24h. Gene expression of TNF-alpha and IL-6 was analyzed by real-time quantitative PCR. |
Reaction Conditions | 20μM; 24h |
Applications | Bifenthrin increased the expression of IL-6 and TNF-alpha mRNA in primary microglia. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | The animals were exposed daily to Bifenthrin via a 0.3 mL intraperitoneal injection of the appropriate concentration in corn oil. After a 7-day treatment period, the livers were collected for analysis. |
Dosage form | 2, 4, 8mg/kg; 7d; i.p. |
Applications | Bifenthrin resulted in a concentration-dependent increase in mitochondrial ROS generation. |
References: | |
| Cas No. | 82657-04-3 | SDF | |
| 别名 | 联苯菊酯 | ||
| Canonical SMILES | O=C([C@H]1C(C)(C)[C@H]1/C=C(Cl)/C(F)(F)F)OCC2=C(C)C(C3=CC=CC=C3)=CC=C2 | ||
| 分子式 | C23H22ClF3O2 | 分子量 | 422.87 |
| 溶解度 | DMSO: 100 mg/mL (236.48 mM) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3648 mL | 11.824 mL | 23.6479 mL |
| 5 mM | 473 μL | 2.3648 mL | 4.7296 mL |
| 10 mM | 236.5 μL | 1.1824 mL | 2.3648 mL |
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| % DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的;
2.
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