Nonachlor | 142507-25-3

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 乙烯基卤化物
• 英文名称: Nonachlor
• 英文别名: cis-Nonachlor；1,3,4,5,7,8,9,10,10-nonachlorotricyclo[5.2.1.02,6]dec-8-ene
• CAS: 142507-25-3
• 化学式: C₁₀H₅Cl₉
• 分子量: 444.227
• InChiKey: OCHOKXCPKDPNQU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  0

ADMET

代谢

(14)C-反式-非林丹，占技术级林丹的大约7%，以玉米油单次给药给大鼠。收集粪便和尿液。大部分放射性出现在粪便中，并鉴定为：1,2-二羟基二氢林丹（17.9%），1-羟基-2-林丹（15.4%），林丹氯醇（13.5%），氧化氯丹（4.1%），反式-林丹（0.8%），和1-羟基-2-氯代-2,3-环氧林丹。还有两个未鉴定的化合物和未改变的非林丹……。

(14)C-trans-nonachlor, which comprises about 7% of technical chlordane, was administered to rats in corn oil as a single dose. Feces and urine were collected. The bulk of the radioactivity appeared in the feces and was identified as: 1,2-dihydroxydihydrochlordene (17.9%), 1-hydroxy-2-chlordene (15.4%), chlordene chlorohydrin (13.5%), oxychlordane (4.1%), trans-chlordane (0.8%), and 1-hydroxy-2-chloro-2,3-epoxychlordene. There were two unidentified compounds and unchanged nonachlor ... .

来源:Hazardous Substances Data Bank (HSDB)

代谢

体外研究中，使用人和大鼠肝脏微粒体制备物，发现了反式氯丹、氧化氯丹、氯丹烯氯醇和1,2-二羟基二氢氯丹。在使用人肝脏制备物时，代谢物的水平非常低。这与在人组织中发现的反式九氯作为主要的氯丹残留物相一致。

In vitro studies with human and rat liver microsomal preparations showed the presence of trans-chlordane, oxychlordane, chlordene chlorohydrin, and 1,2-dihydroxydihydrochlordene. With human liver preparations, the level of metabolites was very low. This correlates with the finding of trans-nonachlor as the major chlordane residue found in human tissues ... .

来源:Hazardous Substances Data Bank (HSDB)

代谢

河流鱼类，如斑节对虾（Leiostomus xanthurus），被暴露在技术级七氯中24天。七氯、t-氯丹、顺式氯丹和非氯丹，这些在技术级七氯中存在的物质，在可食用鱼组织中累积。七氯环氧物形成并也被累积……。

The estuarine fish, spot (Leiostomus xanthurus), was exposed to technical heptachlor for 24 days. Heptachlor, t-chlordane, cis-chlordane, and nonachlor, which were present in the technical grade heptachlor, accumulated in edible fish tissue. Heptachlor epoxide formed and was also accumulated ... .

来源:Hazardous Substances Data Bank (HSDB)

代谢

老鼠被喂食含有10 ppm技术级氯丹的饮食，持续28天。然后对各种氯丹化合物的排泄进行了32天的跟踪。使用电子捕获、负离子化质谱法，结合毛细管气相色谱，测量了21只老鼠脂肪组织中技术级氯丹的14种成分或代谢物的浓度。两种主要八氯异构体，即伽马-氯丹和阿尔法-氯丹的半衰期分别确定为7.1天和5.9天。非氯代的半衰期为9.7天（顺式-非氯代）、14.3天（反式-非氯代）和54.1天（非氯代III）。排泄速率似乎受到分子三个结构特征的控制；环1上氯的总数和构型以及碳2上的氯数目。

Rats were fed a diet containing 10 ppm of technical chlordane for 28 days. The depuration of the various chlordane compounds was then followed for 32 days. The concn of 14 components or metabolites of technical chlordane were measured in the adipose tissues of 21 rats, using electron capture, negative ionization mass spectrometry, coupled with capillary gas chromatography. The half-lives of the two major octachloro isomers, gamma- and alpha-chlordane, were determined to be 7.1 and 5.9 d respectively. The half-lives of the nonachlors were 9.7 (cis-nonachlor), 14.3 (trans-nonachlor), and 54.1 days (nonachlor III). The depuration rates seem to be controlled by three structural features of the molecules; the total number and configuration of the chlorines on ring 1 and the number of chlorines on carbon 2.

来源:Hazardous Substances Data Bank (HSDB)

代谢

有机氯杀虫剂氯丹对人体的毒性影响进行了比较...。对血液中氯丹代谢物进行分析，结果显示按下降顺序存在反式非氯、氧氯丹、肝氯环氧物和顺式非氯。工人血清中氯丹及其代谢物的总范围为9.84 : 4.47 ng/g。还发现害虫控制操作员的血清甘油三酯、肌酸磷酸激酶和乳酸脱氢酶活性也较高...

The toxic effects of the organochlorine insecticide chlordane were compared in man... . Analysis of blood for chlordane metabolites showed their presence in the descending order of trans-nonachlor, oxychlordane, hepatachlorepoxide and cis-nonachlor. The total range of chlordane and its metabolites in the sera of workers was 9.84 : 4.47 ng/g. Serum levels of triglycerides, creatine phosphokinase and lactate dehydrogenase activities were also found to be higher in pest control operators ...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 副作用

其他毒物 - 有机氯

Other Poison - Organochlorine

来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases

毒理性

• 解毒与急救

治疗是对症和支持性的。油类不应作为泻药或皮肤清洁剂使用，因为它们会增加吸收。对于摄入，建议进行洗胃和使用活性炭和硫酸钠。如果发生皮肤接触，应去除受污染的衣物，并用肥皂和水彻底清洁皮肤。儿童和成人的癫痫管理使用的是安定或苯巴比妥。尤其是在儿童中同时使用安定和苯巴比妥时，可能会出现呼吸抑制甚至呼吸停止。这些药物最好只在可以进行紧急气管插管的重症监护区使用。/建议/在有机氯中毒的患者中不使用肾上腺素，因为有机氯化物会引起心肌兴奋性和室性心律失常。然而，在输液无效的低血压情况下可能需要使用多巴胺，在心肺骤停的情况下可能需要使用肾上腺素。... /有机氯杀虫剂/

Treatment is symptomatic and supportive. Oils should not be used as either cathartics or dermal cleansing agents, as they increase absorption. Gastric lavage and use of activated charcoal and sodium sulfate are indicated for ingestion. If dermal exposure occurred, contaminated clothes should be removed, and the skin should be thoroughly cleansed with soap and water. Management of seizures in both children and adults is with Valium or phenobarbital. Respiratory depression and even respiratory arrest, especially with concomitant use of Valium and phenobarbital in children, may occur. These drugs preferably should be used only in critical care areas where emergency endotracheal intubation can be performed. /It is recommended/ that epinephrine not be utilized in patients with organochlorine poisoning, as the organochlorines induce myocardial irritability and ventricular arrhythmias may occur. However, dopamine may be necessary in the event of hypotension unresponsive to fluid administration, and epinephrine may be necessary in the event of cardiopulmonary arrest. ... /Organochlorine insecticides/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

癫痫、低氧血症以及由此引起的酸中毒是直接危及生命的紧急情况。地西泮是首选的抗惊厥药。中到重度中毒患者应该建立静脉通道并使用心脏监护仪。大多数有机氯杀虫剂含有有机溶剂，这些都是严重的吸入危险。皮肤去污染（移除被污染的衣物，用水和绿色或温和的肥皂清洗区域）是必要的，以防止持续的皮肤吸收。小心不要交叉污染医务人员。使用考来烯胺（每天四次，每次3-8克）可以将氯苯酮的粪便排泄量增加七倍，并将平均血半衰期从165天减少到80天。在有机氯化合物暴露中，对于那些有大量肠肝循环的化合物，活性炭也可以减少半衰期，并且在中到重度急性中毒时应该考虑连续剂量。由于广泛的组织结合和大量的分布体积，透析、利尿和血液灌注无效。/有机氯化物/

Seizures, hypoxemia, and resultant acidosis are the immediate life-threatening emergencies. Diazepam is the anticonvulsant of choice. Moderately to severely poisoned patients should have intravenous lines and a cardiac monitor. ...Most organochlorine insecticdes contain organic solvents, which are severe aspiration hazards. Skin decontamination (removal of contaminated clothes, washing of area with water and green or mild soap) is necessary to prevent continued dermal absorption. Be careful not to cross-contaminate health personnel. The use of cholestyramine (3-8 g four times a day) increased fecal excretion of chlordecone by seven times and reduced the mean blood half-life from 165 to 80 days. In organochlorine exposures to compounds that have substantial enterohepatic recirculation, activated charcoal also may reduce the half-life and should be considered in serial doses for moderate to severe acute poisonings. Dialysis, diuresis, and hemoperfusion are ineffective because of extensive tissue binding and large volumes of distribution. /Organochlorines/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

治疗：快速作用的巴比妥类药物或地西泮可能有助于控制抽搐，但必须小心，不要加重任何呼吸抑制。可能需要进行氧疗和人工通气。避免使用肾上腺素。由于没有已知的特定解毒剂，对症治疗必须伴随完全休息。使用适量的肥皂和水清洗皮肤上溢出的任何化合物。如果溅入眼睛，请用水反复冲洗。/氯丹/

Treatment: A rapidly acting barbiturate or diazepam may aid in controlling convulsions, but care must be taken not to augment any respiratory depression. Oxygen therapy and artificial ventilation may be necessary. Avoid epinephrine. Since no specific antidotes are known, symptomatic therapy must be accompanied by complete rest. Use soap and water in adequate quantities to wash off any compound spilled on the skin. If spilled in eyes, wash repeatedly with water. /Chlordane/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

有机氯杀虫剂通过任何途径高度暴露的人员应被观察是否有感觉异常、协调性障碍、言语不清、精神异常和不自主的 motor 活动等警告性癫痫即将发作的症状。如果发生癫痫，将受害者置于左侧卧位，头部向下。移开可能造成伤害的家具或其他固体物品。如果下巴动作剧烈，将衬垫的压舌板放在牙齿之间以保护舌头。尽可能取下假牙和其他可移动的牙齿修复物。吸出口腔和咽喉分泌物，并在可能的情况下，插入一个口咽气道以保持舌头不被阻塞的开放通道。尽量减少噪音和任何可能触发癫痫活动的患者操作。通过面罩给予氧气。在呼吸受到抑制时，通过机械辅助通气来维持肺气体交换。/固体有机氯杀虫剂/

Persons exceptionally exposed to organochlorine pesticides by any route should be observed for sensory disturbances, incoordination, speech slurring, mental aberrations, and involuntary motor activity that would warn of imminent convulsions. If convulsions occur, place the victim in the left lateral decubitus position with the head down. Move away furniture or other solid objects that may be a source of injury. If jaw movements are violent, place padded tongue blades between the teeth to protect the tongue. Whenever possible, remove dentures and other removable dental work. Aspirate oral and pharyngeal secretions, and, when possible, insert an oropharyngeal airway to maintain an open passage unobstructed by the tongue. Minimize noise and any manipulation of the patient that may trigger seizure activity. Administer oxygen by mask. Maintain pulmonary gas exchange by mechanically assisted ventilation whenever respiratin is depressed. /Solid organochlorine insecticides/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

非对称九氯，作为技术级氯丹的主要成分之一，是一个重要的化合物，因为它已知会在人体内累积。

Trans-nonachlor, one of the major constituents of technical chlordane, is an important compound, since it is known to accumulate in humans ... . /trans- Nonachlor/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

有机氯化物从肺部、胃肠道和皮肤被很好地吸收。

Organochlorines are well absorbed from the lung, gastrointestinal tract, and skin. /Organochlorines/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

主要排泄途径是胆汁，尽管几乎所有有机氯化合物都会产生可测量的尿液代谢物。许多未经代谢的杀虫剂被肠道有效重吸收（肠肝循环），从而大大减缓了粪便排泄。/固体有机氯杀虫剂/

The chief route of excretion is biliary, although nearly all organochlorines yield measurable urinary metabolites. ... Many of the unmetabolized pesticides are efficiently reabsorbed by the intestine (enterohepatic circulation) substantially retarding fecal excretion. /Solid organochlorine insecticides/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

有机氯杀虫剂确实会出现在母乳中。/有机氯/

Organochlorine insecticides ... do appear in breast milk. /Organochlorines/

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• [EN] PFKFB3 INHIBITORS AND THEIR USES<br/>[FR] INHIBITEURS DE PFKFB3 ET LEURS UTILISATIONS
  申请人：GERO DISCOVERY LLC

  公开号：WO2020080979A1

  公开（公告）日：2020-04-23

  This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventiions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

  这项披露涉及新的邻苯二甲酰亚胺和异吲哚酮衍生物以及其他PFKFB3抑制剂，用于治疗疾病。该发明还涉及含有此类PFKFB3抑制剂的药物组合物，其制备方法，作为治疗剂的使用方法，以及用于治疗的药物的制备方法，以及包含此类PFKFB3抑制剂的工具包和其他发明。这些PFKFB3抑制剂对于治疗和预防癌症、神经退行性疾病、自身免疫疾病、炎症性疾病、多发性硬化症、代谢性疾病、抑制血管生成以及其他疾病和情况具有用途，在这些情况下，PFKFB3和/或PFKFB4的调节具有益处，以及神经保护作用。
• Instruments for detecting low-molecular weight substance
  申请人：Mizukami Haruki

  公开号：US20050148097A1

  公开（公告）日：2005-07-07

  To provide the following instruments 1 and 2 as a low-molecular-weight substance detection instrument employing immunochromatography capable of detecting conveniently and sensitively detecting a low-molecular weight substance such as an environmental pollutant (e.g., a dioxin), as a target substance contained in a test sample: 1. an instrument, which comprises 1) a test sample application section with which a test sample is brought into contact; 2) a label product reaction section containing a label product containing, as a portion thereof, an antibody capable of binding to a target substance contained in the test sample, the label product being not bound to the reaction section; 3) an unbound label product capturing section containing an element capable of capturing the label product which is not bound to the target substance, the element being bound to the capturing section; and 4) a detection section containing a detection element which, when coming into contact with the target substance bound to the label product, causes a visually observable change, and 2. an instrument wherein a test sample is reacted with a labeled antibody containing, as a portion thereof, an antibody capable of binding to a target substance contained in the test sample, and the resultant reaction product is employed for detecting the target substance contained in the test sample.

  提供以下仪器1和2作为低分子量物质检测仪器，采用免疫层析技术，能够方便敏感地检测低分子量物质，例如环境污染物（例如二恶英），作为测试样品中包含的目标物质：1. 仪器，包括1）测试样品应用部分，用于将测试样品接触；2）标签产物反应部分，包含一种标签产物，其中包含一种能够结合到测试样品中的目标物质的抗体，标签产物未结合到反应部分；3）未结合标签产物捕获部分，包含一种能够捕获未结合到目标物质的标签产物的元素，该元素与捕获部分结合；以及4）检测部分，包含一种检测元素，当与结合到标签产物的目标物质接触时，会引起可视的变化；2. 仪器，其中测试样品与标记抗体反应，其中一部分包含能够结合到测试样品中的目标物质的抗体，产生的反应产物用于检测测试样品中包含的目标物质。
• METHOD AND BIOSENSOR FOR DETECTING ANTIGEN
  申请人：EBARA CORPORATION

  公开号：EP1143251A1

  公开（公告）日：2001-10-10

  A sensor chip for surface plasmon resonance which has a thin metal film, an antibody against a substance with the steroid skeleton such as a steroid hormone, a sex hormone or an environmental hormone (excluding triazine compounds), and a fixation layer for fixing the antibody to the thin metal film; and a method for detecting an environmental hormone which involves the step of exposing the antibody in the above-mentioned sensor chip to a sample, the step of irradiating the thin metal film with light and the step of determining the intensity of the light reflected by the thin metal film. This method achieves a high sensitivity and an excellent selectivity.

  一种用于表面等离子体共振的传感器芯片，它具有一层金属薄膜，一种针对类固醇激素、性激素或环境激素（不包括三嗪化合物）等具有类固醇骨架的物质的抗体，以及一层用于将抗体固定在金属薄膜上的固定层；以及一种检测环境激素的方法，它包括将上述传感器芯片中的抗体暴露在样品中的步骤、用光照射金属薄膜的步骤和测定金属薄膜反射光强度的步骤。这种方法灵敏度高，选择性好。
• Method of removing exogenous endocrine-disrupting chemical in water
  申请人：Hitachi Plant Engineering & Construction Co., Ltd.

  公开号：EP1227065A2

  公开（公告）日：2002-07-31

  Biological treatment for an environmental hormone in water can be efficiently performed by use of a microorganism-immobilized carrier is provided. To biologically remove an environmental hormonal substance in water by a microorganism-immobilized carrier having microorganism immobilized onto a carrier. The microorganism-immobilized carrier is formed of an immobilizing material prepared by mixing and polymerizing a hydrophilic prepolymer and a hydrophobic prepolymer or prepared by polymerizing a prepolymer having a hydrophilic group and a hydrophobic group in a molecule.

  通过使用微生物固定化载体，可以有效地对水中的环境激素进行生物处理。利用微生物固定载体对水中的环境激素物质进行生物去除，该载体上固定有微生物。微生物固定化载体由亲水性预聚物和疏水性预聚物混合聚合制备的固定化材料形成，或由分子中具有亲水基团和疏水基团的预聚物聚合制备的固定化材料形成。
• DRUGS, DRINKS OR FOODS
  申请人：Takara Shuzo Co, Ltd.

  公开号：EP1232756A1

  公开（公告）日：2002-08-21

  Remedies or preventives for diseases caused by the binding of agonists (endocrine disruptors, etc.) to the estrogen receptor, characterized by containing, as the active ingredient, antagonists such as catechins (for example, epigallocatechin gallate) having the antagonism to the estrogen receptor agonists.

  治疗或预防因激动剂（内分泌干扰素等）与雌激素受体结合而引起的疾病的药物，其特征是含有拮抗剂，如儿茶素（例如表没食子儿茶素没食子酸酯）作为活性成分，具有拮抗雌激素受体激动剂的作用。

表征谱图