metofluthrin | 240494-71-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: metofluthrin
• 英文别名: [4-(methoxymethyl)-2,3,5,6-tetrafluorophenyl]methyl (1R)-trans-2,2-dimethyl-3-((Z)-1-propenyl)cyclopropanecarboxylate；Metofluthrin, trans-(Z)-；[2,3,5,6-tetrafluoro-4-(methoxymethyl)phenyl]methyl (1R,3R)-2,2-dimethyl-3-[(Z)-prop-1-enyl]cyclopropane-1-carboxylate
• CAS: 240494-71-7
• 化学式: C₁₈H₂₀F₄O₃
• 分子量: 360.349
• InChiKey: KVIZNNVXXNFLMU-DUVUQDDDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  7

ADMET

代谢

雄性Sprague-Dawley大鼠以1 mg/kg/天的剂量给予(Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ（批号：RIS2001-003，比放射性：6.19 Mbq/mg；放射化学纯度：(12/00) 99.4%；研究中重新纯化两次，(5/7/02) 99.2%，(5/17/02) 99.1%）。给药准备中补充了未标记的S-1264RTZ（/甲氧氟氰/ 批号：010621G，纯度：99.3%）。在排泄研究中，三只动物每天通过灌胃给药21天，收集尿液和粪便样本，持续21天，并在最后一次给药后的24、48和72小时以及5、7、10和14天收集。在组织分布研究中，12只动物通过灌胃给药，并在给药10、16和21次以及最后一次给药后7天，每次三个动物的时间点处死。在排泄研究中，总给药剂量的75%通过尿液排出，22%通过粪便排出。...根据分离的代谢物，主要的代谢途径是酯键的断裂，分子中苄基上的甲基氧化形成醇、醛和羧酸代谢物，分子中酸部分的双键还原，以及形成谷胱甘肽和硫酸酯加成物。/Z-异构体/

Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study, (5/7/02) 99.2%, (5/17/02) 99.1%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 75% of the total administered dose was excreted in the urine and 22% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups on the benzyl moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione and sulfate adducts. /Z-isomer/

来源:Hazardous Substances Data Bank (HSDB)

代谢

雄性Sprague-Dawley大鼠接受1 mg/kg/天的(Carbonyl-(14)C) S-1264RTZ（/甲氧氟脒/，批号RIS2000-019，比放射性：6.50 Mbq/mg；放射化学纯度：(12/00) 99.4%；研究期间重新纯化两次；(5/8/02) 98.6%，(5/16/02) 99.7%）的处理。给药准备中补充了未标记的S-1264RTZ（批号010621G，纯度：99.3%）。在排泄研究中，三只动物每天通过灌胃方式口服实验材料，连续21天，收集尿液和粪便样本，直至21天，并在最后一次给药后24、48、72小时以及5、7、10和14天收集样本。在组织分布研究中，12只动物通过灌胃方式口服实验材料，并在给药10、16、21次和最后一次给药后7天，每个时间点处死3只动物。在排泄研究中，总给药剂量的57%通过尿液排出，38%通过粪便排出。根据分离的代谢物，主要的代谢途径包括酯键的断裂，分子中酸部分甲基基团的氧化形成醇、醛和羧酸代谢物，酸部分双键的还原，以及形成谷胱甘肽、硫酸酯和葡萄糖醛酸加合物。/Z-异构体/

Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Carbonyl-(14)C) S-1264RTZ (/metofluthrin/ lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study;(5/8/02) 98.6%, (5/16/02) 99.7%),. Dosing preparations were supplemented with unlabeled S-1264RTZ (lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 57% of the total administered dose was excreted in the urine and 38% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/

来源:Hazardous Substances Data Bank (HSDB)

代谢

Sprague-Dawley 大鼠，无论雌雄，被用 1 或 20 毫克/千克剂量的 (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ（/甲氧氟菊酯 Z-异构体/ 批号 RIS2001-003，比放射性：6.19 Mbq/毫克；放射化学纯度：(12/00) 99.4%；在研究中重新精制 4 次，(10/22/01) 99.1%，(10/31/01) 98.6%，(11/19/01) 99.1%，(11/26/01) 99.5%）处理。给药制剂中补充了未标记的 S-1264RTZ（/甲氧氟菊酯 Z-异构体/ 批号 010621G，纯度：99.3%）。在排泄研究中，每个性别/组各四只动物通过灌胃口服给予 1 或 20 毫克/千克的试验材料，并在给药后长达 7 天内收集尿液和粪便样本。空气样本在 72 小时内收集。在药代动力学研究中，每个性别/组各三只动物被给予 1 或 20 毫克/千克的试验材料，并在给药后指定的时间间隔内抽取血液样本，直至 7 天。在组织分布研究中，每个性别/组各 12 只动物被给予 1 或 20 毫克/千克的试验材料，并在给药后指定的时间间隔处死每组各 3 只动物，并测定特定组织中放射性标记的浓度。在排泄研究中，给予剂量的 60 至 71% 通过尿液排出，25 至 36% 通过粪便排出，两个剂量水平之间几乎没有差异。...根据分离出的代谢物，代谢的主要途径是酯键的断裂，分子中酸部分甲基氧化形成醇、醛和羧酸代谢物，酸部分双键的还原，以及形成谷胱甘肽、硫酸盐和葡萄糖苷酸缀合物。/Z-异构体/

Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (10/22/01) 99.1%, (10/31/01) 98.6%, (11/19/01) 99.1%, (11/26/01) 99.5%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 60 to 71% of the administered dose was excreted in the urine and 25 to 36% in the feces with little difference demonstrated between the two dosing levels. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/

来源:Hazardous Substances Data Bank (HSDB)

代谢

Sprague-Dawley 大鼠和雌性大鼠分别给予1或20毫克/千克的(Carbonyl-(14)C) S-1264RTE(顺式异构体/批号RIS2000-020，比活度：6.50 Mbq/mg；放射化学纯度：(12/00) 99.2%；在实验过程中重新精制4次，(3/18/02) 99.0%，(3/26/02) 98.1%，(4/15/02) 99.4%，(4/22/02) 99.2%；）。投药制剂中补充了未标记的S-1264RTE(顺式异构体/批号010831G，纯度：96.9%)。在排泄研究中，每组4只/性别的大鼠通过灌胃给予1或20毫克/千克的试验物质，并在给药后7天内收集尿液和粪便样本。空气样本在72小时内收集。在胆汁排泄研究中，将胆管插管的4只雄性大鼠给予1毫克/千克的试验物质。在给药后72小时内收集胆汁、尿液和粪便样本。在药代动力学研究中，每组3只/性别的大鼠给予1或20毫克/千克的试验物质，并在给药后7天内每隔特定时间抽取血液样本。在组织分布研究中，每组12只/性别的大鼠给予1或20毫克/千克的试验物质，并在给药后特定时间点每组3只/性别的大鼠处死，并测定特定组织中放射性标记的浓度。在排泄研究中，29至45%的给药剂量通过尿液排出，50至66%通过粪便排出，两个剂量水平之间几乎没有差异。...根据分离出的代谢物，代谢的主要途径是酯键的断裂，分子中酸部分甲基氧化形成醇、醛和羧酸代谢物，酸部分双键的还原，以及硫酸盐加合物的形成。/E-异构体/

Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTE (/metofluthrin e-isomer/ lot no. RIS2000-020, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.2%; repurified 4 times during study, (3/18/02) 99.0%, (3/26/02) 98.1%, (4/15/02) 99.4%, (4/22/02) 99.2%;). Dosing preparations were supplemented with unlabeled S-1264RTE (/metofluthrin e-isomer/ lot no. 010831G, purity: 96.9%) . In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 29 to 45% of the administered dose was excreted in the urine and 50 to 66% in the feces with little difference demonstrated between the two dosing levels. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of a sulfate adduct. /E-isomer/

来源:Hazardous Substances Data Bank (HSDB)

代谢

斯普拉格-道利雄性和雌性大鼠分别用1或20 mg/kg的(羰基-(14)C) S-1264RTZ (甲氧氟虫腈Z-异构体/批号RIS2000-019，比活度：6.50 Mbq/mg；放射化学纯度：(12/00) 99.4%；在研究中重新纯化4次，(12/3/01) 99.6%，(12/19/1) 98.2%，(2/18/02) 98.6%，(2/25/02) 98.9%)进行处理。给药准备中补充了未标记的S-1264RTZ (甲氧氟虫腈Z-异构体/批号010621G，纯度：99.3%)。 在排泄研究中，每组每性别四只动物通过灌胃给予1或20 mg/kg的测试材料，并在给药后7天内收集尿液和粪便样本。空气样本收集了72小时。在胆汁排泄研究中，四只雄性大鼠的胆管被插管后，给予1 mg/kg的测试材料。在给药后72小时内收集胆汁、尿液和粪便样本。在药代动力学研究中，每组每性别三只动物给予1或20 mg/kg的测试材料，并在给药后指定的时间间隔内抽取血液样本，直至7天。在组织分布研究中，每组每性别12只动物给予1或20 mg/kg的测试材料，并在给药后指定的时间点每组每性别三只动物被安乐死，并测定特定组织中放射性标记的浓度。 在排泄研究中，给予剂量的44至57%通过尿液排出，38至52%通过粪便排出，两个给药水平之间差异不大。空气采样回收了0.7至1.4%的给予剂量。在给药后第一个24小时内回收了74至83%的给予剂量。在胆汁排泄研究中，30至40%的剂量在胆汁中回收，25至26%在尿液中回收，30至39%在粪便中回收。 根据分离的代谢物，主要的代谢途径包括酯键的断裂，分子中酸部分的甲基氧化形成醇、醛和羧酸代谢物，酸部分中双键的还原，以及形成谷胱甘肽、硫酸酯和葡萄糖醛酸加成物。/Z-异构体/

Sprague-Dawley rats of both sexes were treated with 1 or 20 mg/kg of (Carbonyl-(14)C) S-1264RTZ (/metofluthrin z-isomer/ lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 4 times during study, (12/3/01) 99.6%, (12/19/1) 98.2%, (2/18/02) 98.6%, (2/25/02) 98.9%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin z-isomer/ lot no. 010621G, purity: 99.3%). In the Excretion Study, four animals/sex/group were dosed orally by gavage with 1 or 20 mg/kg of the test material and urine and fecal samples were collected up to 7 days post-dose. Air samples were collected through 72 hours. In the Biliary Excretion Study, four male rats, whose bile ducts had been cannulated, were dosed with 1 mg/kg of the test material. Bile, urine and fecal samples were collected through 72 hours post-dose. In the Pharmacokinetics Study, 3 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and blood samples were drawn at specified time intervals up to 7 days post-dose. In the Tissue Distribution Study, 12 animals/sex/group were dosed with 1 or 20 mg/kg of the test material and 3 animals/sex/group/time point were euthanized at specified time intervals post-dose and the concentration of radiolabel in particular tissues was determined. In the Excretion Study, 44 to 57% of the administered dose was excreted in the urine and 38 to 52% in the feces with little difference demonstrated between the two dosing levels. Air sampling recovered from 0.7 to 1.4% of the administered dose. Seventy four to 83% of the administered dose was recovered in the 1st 24 hours post-dose. In the Bile Excretion Study, 30 to 40% of the dose was recovered in the bile, 25 to 26% in the urine and 30 to 39% in the feces. ... Based upon the isolated metabolites, the major pathways of metabolism were cleavage of the ester linkage, oxidation of methyl groups in the acid moiety of the molecule to form alcohol, aldehyde and carboxylic acid metabolites, reduction of the double bond in the acid moiety of the molecule, and the formation of glutathione, sulfate and glucuronide adducts. /Z-isomer/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 紧急急救：确保已经进行了充分的中和。如果患者停止呼吸，请开始人工呼吸，最好使用需求阀复苏器、袋阀面罩装置或口袋面罩，按训练操作。如有必要，执行心肺复苏。立即用缓慢流动的水冲洗受污染的眼睛。不要催吐。如果发生呕吐，让患者前倾或将其置于左侧（如果可能的话，头部向下）以保持呼吸道畅通，防止吸入。保持患者安静，维持正常体温。寻求医疗帮助。 /拟除虫菊酯、拟除虫菊酯类和相关化合物/

/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Pyrethrins, pyrethroids, and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 基本治疗：建立专利气道（如有需要，使用口咽或鼻咽气道）。如有必要，进行吸痰。密切观察呼吸不足的迹象，如有必要，进行辅助通气。通过非重复呼吸面罩以10至15升/分钟的速度给予氧气。预期可能出现癫痫，并在必要时进行治疗……对于眼睛污染，立即用水冲洗眼睛。在转运过程中，用0.9%的生理盐水（NS）持续冲洗每只眼睛……不要使用催吐剂。对于摄入，如果患者能够吞咽、有强烈的干呕反射且不流口水，则用水冲洗口腔，并给予5毫升/千克，最多200毫升的水进行稀释。给予活性炭…… . /天然除虫菊酯、拟除虫菊酯及相关化合物/

/SRP:/ Basic treatment: . Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Anticipate seizures and treat if necessary... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Administer activated charcoal ... . /Pyrethrins, pyrethroids, and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

/SRP:/ 高级治疗：对于无意识或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。考虑给予β受体激动剂如沙丁胺醇治疗严重支气管痉挛...。监测心率和必要时治疗心律失常...。开始静脉输注5%葡萄糖水（D5W）/SRP: "保持开放"，最低流速/。如果出现低血容量的迹象，使用0.9%生理盐水（NS）或乳酸钠林格液（LR）。对于伴有低血容量迹象的低血压，谨慎给予液体。注意观察液体过载的迹象...。用地西泮或劳拉西泮治疗癫痫...。使用丙美卡因氢氯化物协助眼部冲洗...。/拟除虫菊酯、拟除虫菊酯类和相关化合物/

/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for air way control in the patient who is unconscious or is in severe respiratory distress. Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias if necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Pyrethrins, pyrethroids, and related compounds/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

皮肤去污。立即用肥皂和水清洗皮肤...。如果出现刺激或感觉异常效应，应通过医生获得治疗。由于拟除虫菊酯的挥发显然是导致面部感觉异常的原因，应采取强烈措施（通风、保护面罩和头罩）以避免蒸汽接触面部和眼睛。维生素E油制剂（dL-α-生育酚醋酸酯）在预防和停止感觉异常反应方面具有独特效果。它们适用于现场条件下的皮肤应用。玉米油也有一定效果，但可能的副作用和持续使用使其不太合适。凡士林的效果不如玉米油。氧化锌实际上会加剧反应。/拟除虫菊酯/

Skin decontamination. Wash skin promptly with soap and water ... . If irritant or paresthetic effects occur, obtain treatment by a physician. Because volatilization of pyrethroids apparently accounts for paresthesia affecting the face, strenuous measures should be taken (ventilation, protective face mask and hood) to avoid vapor contact with the face and eyes. Vitamin E oil preparations (dL-alpha tocopheryl acetate) are uniquely effective in preventing and stopping the paresthetic reaction. They are safe for application to the skin under field conditions. Corn oil is somewhat effective, but possible side effects with continuing use make it less suitable. Vaseline is less effective than corn oil. Zinc oxide actually worsens the reaction. /Pyrethroids/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

眼睛污染。一些拟除虫菊酯化合物可能对眼睛非常腐蚀。应采取特殊措施以避免眼睛污染。眼睛应立即通过大量清洁水或生理盐水长时间冲洗来处理。如果刺激持续，应获得专业的眼科护理。/拟除虫菊酯/

Eye contamination. Some pyrethroid compounds can be very corrosive to the eyes. Extraordinary measures should be taken to avoid eye contamination. the eye should be treated immediately by prolonged flushing of the eye with copious amounts of clean water or saline. If irritation persists, obtain professional ophthalmologic care. /Pyrethroids/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

Sprague-Dawley雄性大鼠以1 mg/kg/天的剂量给予(Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ（批号RIS2001-003，比活度：6.19 Mbq/mg；放化纯度：(12/00) 99.4%；在研究中重新精制2次，(5/7/02) 99.2%，(5/17/02) 99.1%）。给药制剂中补充了未标记的S-1264RTZ（/metofluthrin/批号010621G，纯度：99.3%）。在排泄研究中，三只动物每天通过灌胃给药21天测试材料，并通过21天每天收集尿液和粪便样本，并在最终剂量后24、48和72小时以及5、7、10和14天收集。在组织分布研究中，12只动物通过灌胃给药测试材料，并在10、16和21剂次以及最终剂量后7天每组三只动物安乐死。在排泄研究中，给药总剂量的75%通过尿液排出，22%通过粪便排出。在整个给药期间，肝脏和肾脏是放射性恢复的主要部位，放射性水平在给药期间稳定。在最终剂量后14天，肝脏、红细胞和毛发是放射性恢复的主要位置。在给药期间，从胃、小肠、盲肠和大肠中恢复的放射性水平稳定或略有增加。毛发中放射性恢复在16次给药时达到峰值。放射性没有在脂肪中隔离，也没有显著部分给药剂量通过血脑屏障。... /Z-异构体/

Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Methoxymethylbenzyl-alpha -(14)C) S-1264RTZ (lot no. RIS2001-003, specific radioactivity: 6.19 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study, (5/7/02) 99.2%, (5/17/02) 99.1%). Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 75% of the total administered dose was excreted in the urine and 22% in the feces. The liver and kidneys were the primary sites of radiolabel recovery over the course of the dosing period with the level of radioactivity stabilizing over the dosing period. At 14 days post-final dose, the liver, red blood cell and hair were the primary locations where the radiolabel was recovered. The level of radioactivity recovered from the stomach, small intestine, cecum and large intestine was stabilized or slightly increased over the course of the dosing period. Radiolabel recovered in the hair peaked at the time of the 16th dose. The radiolabel was not sequestered in the fat nor did a significant fraction of the administered dose pass across the blood:brain barrier. ... /Z-isomer/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

实验中，雄性Sprague-Dawley大鼠以1 mg/kg/天的剂量口服给予(Carbonyl-(14)C) S-1264RTZ（批号RIS2000-019，比活度：6.50 Mbq/mg；放射化学纯度：(12/00) 99.4%；在研究中重新精制2次；(5/8/02) 98.6%，(5/16/02) 99.7%），。给药制剂中补充了未标记的S-1264RTZ（/甲氟菊酯/批号010621G，纯度：99.3%）。在排泄研究中，三只动物每天通过灌胃给予实验材料，连续21天，并且每天收集尿液和粪便样本，直到21天以及最后一次给药后的24、48和72小时以及5、7、10和14天。在组织分布研究中，12只动物通过灌胃给予实验材料，每个时间点处死3只动物，分别在第10、16和21次给药后以及最后一次给药后的7天。在排泄研究中，总给药剂量的57%通过尿液排出，38%通过粪便排出。在整个给药期间，肝脏和肾脏是放射标签恢复的主要部位，放射性水平在给药期间稳定。然而，在最后一次给药后的14天，红细胞和毛发成为放射标签恢复的主要位置。胃、小肠、盲肠和大肠中恢复的放射性水平在给药期间稳定。毛发中恢复的放射标签在第21次给药时达到峰值。放射标签没有在脂肪中隔离，也没有显著部分通过血脑屏障。... /Z-异构体/

Male Sprague-Dawley rats were treated with 1 mg/kg/day of (Carbonyl-(14)C) S-1264RTZ (lot no. RIS2000-019, specific radioactivity: 6.50 Mbq/mg; radiochemical purity: (12/00) 99.4%; repurified 2 times during study;(5/8/02) 98.6%, (5/16/02) 99.7%),. Dosing preparations were supplemented with unlabeled S-1264RTZ (/metofluthrin/ lot no. 010621G, purity: 99.3%). In the Excretion Study, three animals were dosed orally by gavage daily for 21 days with the test material and urine and fecal samples were collected up daily through 21 days and at 24, 48, and 72 hours and 5, 7, 10 and 14 days post-final dose. In the Tissue Distribution Study, 12 animals were dosed orally by gavage with the test material and 3 animals/time point were euthanized after 10, 16, and 21 doses and 7 days post-final dose. In the Excretion Study, 57% of the total administered dose was excreted in the urine and 38% in the feces. The liver and kidneys were the primary sites of radiolabel recovery over the course of the dosing period with the level of radioactivity stabilizing over the dosing period. However, at 14 days post-final dose, the red blood cell and hair were the primary locations where the radiolabel was recovered. The level of radioactivity recovered from the stomach, small intestine, cecum and large intestine was stabilized over the course of the dosing period. Radiolabel recovered in the hair peaked at the time of the 21st dose. The radio