Amitraz (BTS-27419)
(Synonyms: 双甲脒; BTS-27419) 目录号 : GC33983
A formamidine acaricide
Cas No.:33089-61-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amitraz is a formamidine acaricide.1 It induces mortality and reduces fecundity in adult R. annulatus when used at a concentration of 300 ppm. It is lethal to adult H. bipinosa (LC50 = 181 ppm). Amitraz (100 ?M) reduces viability of primary rat hippocampal cells.2 In vivo, amitraz (170 mg/kg) increases malondialdehyde (MDA) and nitric oxide (NO) levels and decreases superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPX) activities in rat liver, kidney, brain, spleen, and testis.3 Dietary administration of amitraz reduces larval weight and larval and pupal survival in honey bee (A. mellifera) populations.4
1.Ravindran, R., Jyothimol, G., Amithamol, K.K., et al.In vitro efficacy of amitraz, coumaphos, deltamethrin and lindane against engorged female Rhipicephalus (Boophilus) annulatus and Haemaphysalis bispinosa ticksExp. Appl. Acarol.75(2)241-253(2018) 2.Del Pino, J., Frejo, M.T., Baselga, M.J.A., et al.Impaired glutamatergic and GABAergic transmission by amitraz in primary hippocampal cellsNeurotoxicol. Teratol.5082-87(2015) 3.Kanbur, M., Sili?, Y., Eraslan, G., et al.The toxic effect of cypermethrin, amitraz and combinations of cypermethrin-amitraz in ratsEnviron. Sci. Pollut. Res. Int.23(6)5232-5242(2016) 4.Dai, P., Jack, C.J., Mortensen, A.N., et al.Chronic toxicity of amitraz, coumaphos and fuvalinate to Apis mellifera L. larvae reared in vitroSci. Rep.8(1)5635(2018)
| Cas No. | 33089-61-1 | SDF | |
| 别名 | 双甲脒; BTS-27419 | ||
| Canonical SMILES | CN(/C=N/C1=CC=C(C)C=C1C)/C=N/C2=CC=C(C)C=C2C | ||
| 分子式 | C19H23N3 | 分子量 | 293.41 |
| 溶解度 | DMSO : 50 mg/mL (170.41 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4082 mL | 17.041 mL | 34.082 mL |
| 5 mM | 0.6816 mL | 3.4082 mL | 6.8164 mL |
| 10 mM | 0.3408 mL | 1.7041 mL | 3.4082 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Effects of the pesticide Amitraz and its metabolite BTS 27271 on insulin and glucagon secretion from the perfused rat pancreas: involvement of alpha2D-adrenergic receptors
Metabolism 1999 Nov;48(11):1461-9.PMID:10582558DOI:10.1016/s0026-0495(99)90160-9.
The study purpose was to investigate the direct effect of Amitraz, a formamidine insecticide/acaricide, and its active metabolite BTS 27271 on insulin and glucagon secretion from the perfused rat pancreas. Amitraz and BTS 27271 (0.01, 0.1, 1, and 10 micromol/L) inhibited insulin secretion in a concentration-dependent manner. Amitraz increased glucagon secretion at 10 micromol/L, whereas BTS 27271 increased glucagon secretion at 1 and 10 micromol/L. Amitraz- and BTS 27271-induced decreases in insulin secretion and increases in glucagon secretion were not abolished during the 10-minute washout period. During the arginine treatment, both Amitraz and BTS 27271 groups (0.1, 1, and 10 micromol/L) had lower insulin secretion and higher glucagon secretion than the control group. Idazoxan, an alpha2A/2D-adrenergic receptor (AR) antagonist, prevented the inhibitory effect of Amitraz on insulin secretion in a concentration-dependent manner, but prazosin, an alpha1- and alpha2B/2C-AR antagonist, failed to antagonize the effect of Amitraz. These results demonstrate that (1) Amitraz and BTS 27271 inhibit insulin and stimulate glucagon secretion from the perfused rat pancreas, (2) Amitraz inhibits insulin secretion by activation of alpha2D-ARs, since rats have alpha2D- but not alpha2A-ARs, and (3) Amitraz and BTS 27271 may have a high binding affinity to the alpha2D-ARs of pancreatic islets.
Amitraz poisoning
Indian J Pediatr 2013 Apr;80(4):349-50.PMID:22576295DOI:10.1007/s12098-012-0772-2.
Amitraz is a formamidine insecticide and acaricide which acts on alpha 2-adrenergic receptors. There is little information available in the literature about the toxicity and treatment of poisoning by this compound. The authors report Amitraz poisoning in a 13-y-old boy which was managed with supportive care with a good outcome.
Poisoning with Amitraz
Toxicol Rev 2003;22(2):71-4.PMID:15071816DOI:10.2165/00139709-200322020-00001.
Amitraz, an insecticide and veterinary medicine, has been available in many countries since 1974 but reports of poisoning with it have only become prominent in the last 7 years. The vast majority of cases have occurred in Turkey and have involved children. The data available, both human and animal, do not allow clear separation of the features of toxicity of Amitraz from those of the hydrocarbon solvents in which it is commonly dissolved. Amitraz stimulates alpha 2-adrenoceptors resulting in impairment of consciousness, respiratory depression, convulsions, bradycardia, hypotension, hypothermia and hypoglycaemia. Even the most severely poisoned patients recover with nothing more than intensive care; only one possible death has been documented. Animal studies indicate that the alpha 2-adrenoceptor antagonists, yohimbine and atipamezole, can reverse amitraz-induced toxicity but they have not been assessed in poisoned humans.
Oxidative stress and cell death induction by Amitraz and its metabolite BTS-27271 mediated through cytochrome P450 and NRF2 pathway alteration in primary hippocampal cell
Food Chem Toxicol 2019 Jul;129:87-96.PMID:31029719DOI:10.1016/j.fct.2019.04.042.
Amitraz is a neurotoxic formamidine pesticide that induces cell death in hippocampal neurons, although its mechanisms are unknown. Amitraz produces reactive oxygen species (ROS), which could lead to cell death. Amitraz was shown to induce different cytochrome P450 (CYP) isoenzymes involved with ROS and apoptotic cell death induction. Finally, Amitraz was described to decrease the activity of antioxidant enzymes regulated through KEAP1/NRF2 pathway, thus likely leading to a reduction of ROS elimination and to cell death induction. We evaluated the effect of Amitraz or BTS-27271 co-treatment with or without the antioxidant N-acetylcysteine and/or the unspecific CYP inhibitor 1-aminobenzotriazole on cell viability and its related mechanisms in wild type and silenced primary hippocampal neurons after 24 h treatment. We observed that Amitraz produced oxidative stress and CYPs induction leading to apoptotic cell death. ROS generation was partially mediated by CYPs induction and downregulation of NRF2-pathway through KEAP1 overexpression. These data could help explain the mechanism by which Amitraz induces cell death and oxidative stress and provide a therapeutic strategy to protect against this effect in case of poisoning.
Amitraz, an underrecognized poison: A systematic review
Indian J Med Res 2016 Sep;144(3):348-358.PMID:28139533DOI:10.4103/0971-5916.198723.
Background & objectives: Amitraz is a member of formamidine family of pesticides. Poisoning from Amitraz is underrecognized even in areas where it is widely available. It is frequently misdiagnosed as organophosphate poisoning. This systematic review provides information on the epidemiology, toxicokinetics, mechanisms of toxicity, clinical features, diagnosis and management of Amitraz poisoning. Methods: Medline and Embase databases were searched systematically (since inception to January 2014) for case reports, case series and original articles using the following search terms: 'Amitraz', 'poisoning', 'toxicity', 'intoxication' and 'overdose'. Articles published in a language other than English, abstracts and those not providing sufficient clinical information were excluded. Results: The original search yielded 239 articles, of which 52 articles described human cases. After following the inclusion and exclusion criteria, 32 studies describing 310 cases (151 females, 175 children) of human poisoning with Amitraz were included in this systematic review. The most commonly reported clinical features of Amitraz poisoning were altered sensorium, miosis, hyperglycaemia, bradycardia, vomiting, respiratory failure, hypotension and hypothermia. Amitraz poisoning carried a good prognosis with only six reported deaths (case fatality rate, 1.9%). Nearly 20 and 11.9 per cent of the patients required mechanical ventilation and inotropic support, respectively. The role of decontamination methods, namely, gastric lavage and activated charcoal was unclear. Interpretation & conclusions: Our review shows that Amitraz is an important agent for accidental or suicidal poisoning in both adults and children. It has a good prognosis with supportive management.