CAS: 303-53-7; 3-(5H-Dibenzo[a,D][7]Annulen-5-Ylidene)-N,N-Dimethylpropan-1-Amine
- 英文名称3-(5H-Dibenzo[a,D][7]Annulen-5-Ylidene)-N,N-Dimethylpropan-1-Amine
- 中文名称环苯扎林
- IUPAC名称3-(5H-dibenzo[a,d][7]annulen-5-ylidene)-N,N-dimethylpropan-1-amine
- 其它别名Amrix,Fexmid
- CAS编号303-53-7
- MFCD编号:MFCD00867680
- EINECS号:206-145-8
- FDA UNII编号:69O5WQQ5TI
- 分子式:C20H21N
- 分子量:275.39
- 产品CID: 1288174
- 同类组份化合物CAS303-53-7 (free base)6202-23-9 (HCl)
- 产品分类原料药 → 麻醉剂 → 骨骼肌松弛药
物理性质
- 熔点216-218°C(hydrochloridesalt)
- 沸点405.9 °C at 760 mmHg
- 闪点177.8 °C
- 密度1.096 g/cm3
- pKa:pKa 8.47 (Uncertain)
- PSA:3.24
- LogP:4.5538
- 折射率1.7500 (estimate)
- 蒸汽压2.29X10-6 mm Hg at 25 °C (est)
- 溶解性In water, 1.09 mg/L at 25 °C (est)
- 外观形态固体
- 储存条件Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
- 产品应用该化合物用于一种辅助剂,用来缓解与肌肉严重疾病状况有关的肌肉抽搐.
MSDS等安全信息
- GHS象形图
- GHS符号GHS07;
注释: Exclamation mark - 危险类别急性毒性 类别4(吸入)
急性毒性 类别4(经皮)
急性毒性 类别4(经口)
严重眼刺激 类别2 - 警示词Warning(警告)
- 危险描述H332 |吸入有害.
H312 |皮肤接触有害.
H302 |吞咽有害.
H319 |造成严重眼刺激. - 防范说明P201-P202-P264-P270-P281-P301+P310-P308+P313-P321-P330-P405-P501-
- UN编号2811
- 安全声明IDENTIFICATION AND USE: Cyclobenzaprine (used in the form of cyclobenzaprine hydrochloride tablets) is indicated as an adjunct to rest and physical therapy for relief of muscle spasm associated with acute, painful musculoskeletal conditions. HUMAN EXPOSURE AND TOXICITY: Manifestations of toxicity may develop rapidly after a cyclobenzaprine overdose, and rarely, death may occur. The most common toxic effects associated with cyclobenzaprine overdose are drowsiness and tachycardia; less frequent manifestations include tremor, agitation, coma, ataxia, hypertension, slurred speech, confusion, dizziness, nausea, vomiting, and hallucinations. Rarely, potentially serious effects may include cardiac arrest, chest pain, cardiac dysrhythmias, severe hypotension, seizures, and neuroleptic malignant syndrome. Serotonin syndrome is another potential side effect. Blood concentration of > or = 0.8 mg/L cyclobenzaprine may be associated with a fatal outcome. In one case of accidental overdose, the victim developed severe hypothermia and then developed cardiac arrest during transport. ANIMAL STUDIES: Ptyalism, emesis, tremors, convulsions and increased respiratory rate developed and death occurred within 1 hour following single oral doses of 180 mg/kg or more by gavage in dogs. Acute exposure to the drug in rats resulted in ataxia, decreased respiratory rate, sedation, flaccid hind legs, loss of the ear flick reflex, loss of the righting reflex with swimming movements, intermittent clonic convulsions, weight loss, lethargy, and then death. The drug was more toxic to infant and weanling rats than to young adults. In rats treated with cyclobenzaprine hydrochloride for up to 67 weeks at doses of approximately 5 to 40 times the maximum recommended human dose, pale, sometimes enlarged, livers were noted and there was a dose-related hepatocyte vacuolation with lipidosis. No evidence of embryo lethality or teratogenicity was revealed following oral doses of 5, 10 or 20 mg/kg/day in studies in mice and rabbits. The reproductive performance and fertility of males and females, and the growth and survival of their offspring were not adversely affected by doses of 5 or 10 mg/kg/day in rats. Litter size, size and survival of the pups, and weight gain of the mothers were decreased by doses of 20 mg/kg/day. Cyclobenzaprine hydrochloride was determined to have no genotoxic effects in several assays, including mouse bone marrow micronucleus assay; Salmonella-Escherichia coli mammalian microsome reverse mutation assay with confirmatory assay; and in a CHO cells chromosomal aberration assay with and without metabolic activation. | Cyclobenzaprine is structurally and pharmacologically related to tricyclic antidepressants. Among the most dreaded toxicities linked with cyclical antidepressants, overdoses affect fast-acting sodium channels in the cardiac conduction system. Cyclical antidepressants block the cardiac sodium channel and cause prolongation of cardiac depolarization, which manifests as QRS widening on electrocardiograms. There is also evidence that cyclical antidepressants may decrease the seizure threshold by interfering with chloride conductance on the GABA receptor. | One study retrospectively looked at 750 charts at five regional poison centers between the years 1989 to 1993. Based on their retrospective study, the authors concluded that cyclobenzaprine in toxic doses less than 1000 mg does not appear to produce the life-threatening neurotoxicity and cardiotoxic dysrhythmias associated with traditional tricyclic antidepressants. The case report of cyclobenzaprine toxicity describes ileus and simultaneous ST segment elevations on EKG. | Other case reports, however, have implicated cyclobenzaprine in acute overdose as the culprit leading to fatalities. For example, there were two reported cases of overdoses in which elevated levels of cyclobenzaprine were found in postmortem evaluations of the patients. The authors, therefore, document an association linking elevated cyclobenzaprine levels with two examples of presumed fatal overdoses. | The most common effects associated with cyclobenzaprine overdose are drowsiness and tachycardia. Rare but potentially critical manifestations of overdose are cardiac arrest, cardiac dysrhythmias, severe hypotension, seizures, and neuroleptic malignant syndrome. Changes in the electrocardiogram, particularly in the QRS axis or width, are clinically significant indicators of cyclobenzaprine toxicity. | To summarize, treatment beyond GI decontamination is unnecessary for less than 100 mg ingestions. Cyclobenzaprine does not appear to produce life-threatening cardiovascular or neurologic effects in doses less than 1000 mg, and serious toxicity such as arrhythmias, hypotension, and seizures occur at doses greater than 1000 mg. | Although rare, deaths may occur from overdosage(>1000 mg) with cyclobenzaprine. As management of overdose is complex, the clinician should contact a poison control center for the latest information on treatment. | Management of Toxicity | * General measures include airway breathing and circulation | * To protect against potentially critical arrhythmias, obtain an EKG and quickly initiate cardiac monitoring | * Protect the patient’s airway, and establish an intravenous line | * Gastrointestinal Decontamination by large volume gastric lavage followed by activated charcoal | * Serum alkalinization using sodium bicarbonate if EKG exhibits QRS prolongation | * Dysrhythmias unresponsive to sodium bicarbonate and hyperventilation may respond to phenytoin, lidocaine, or bretylium | * In patients with CNS depression, early intubation because of the potential for sudden collapse | * Seizures control with benzodiazepines or, if these are ineffective, other anticonvulsants (e.g., phenobarbital, phenytoin) | * Physostigmine administration should be in close consultation with a poison control center
欧盟法规
ECHA物质C&L通报REACH预注册上下游产品
CAS号6682-26-4 Cyclobenzaprine... | CAS号18029-54-4 5-[3-(二甲基氨基)丙基]... | CAS号109-54-6 3-氯-1-(N,N-二甲基)丙胺 | CAS号2222-33-5 5-二苯并环庚烯酮 | CAS号6682-26-4 Cyclobenzaprine...合成工艺路线路线简述
环苯扎林 N-氧化物置于sodium Tetrahydroborate体系中,用 水 用作溶剂,以92%的收率获得环苯扎林
参考文献:A Chemoselective Deoxygenation Of N-Oxides By Sodium Borohydride-raney Nickel In Water
标题:A Chemoselective Deoxygenation Of N-Oxides By Sodium Borohydride-raney Nickel In Water
摘要:A Simple And Convenient Protocol For Deoxygenation Of Aliphatic And Aromatic N-Oxides To The Corresponding Amines In Good To Excellent Yield Using Sodium Borohydride-Raney Nickel In Water Is Reported. Other Functional Moieties Such As Alkenes,Halides,Ethers,And Amides Are Unaffected Under The Present Reaction Condition. (C) 2010 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tetlet.2010.08.045
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2902500000-苯乙烯
2902600000-乙苯 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
专利号:US-2008227851-A1
优先权日:2007-03-12
标题 :Laulimalide and laulimalide analogs
发明人：WENDER PAUL A
权利人:WENDER PAUL A
摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.
专利号:US-2005282898-A1
优先权日:2004-06-01
标 题 :Methods for the synthesis of milnacipran and congeners thereof
专利号:EP-4630405-A1
优先权日:2022-12-06
标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels
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供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Khan I, Kahwaji CI. Cyclobenzaprine. 2020 Aug 10. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan–. 2012–. Cyclobenzaprine. 2017 Jan 30. 93(3):Online. 2015 Feb 23. 314(15):1572-80. doi: 10.1001/jama.2015.13043. 2006–. Cyclobenzaprine. 2020 Jul 20. 76(2):318-328. doi: 10.1136/annrheumdis-2016-209724. Epub 2016 Jul 4. 48(4):15-19.
9: Bulbena-Cabre A, Dunn NR, Swift RG. Cyclobenzaprine-Induced Hallucinosis. Prim Care Companion CNS Disord. 2015 Jun 25;17(3):10.4088/PCC.14l01773. doi: 10.4088/PCC.14l01773.
10: Leite FM, Atallah AN, El Dib R, Grossmann E, Januzzi E, Andriolo RB, da Silva EM. Cyclobenzaprine for the treatment of myofascial pain in adults. Cochrane Database Syst Rev. 2009 Jul 8;2009(3):CD006830. doi: 10.1002/14651858.CD006830.pub3.
合成参考文献
参考文献:10.3389/fphar.2011.00017
摘要:Smith HS, Bracken D, Smith JM. Pharmacotherapy for fibromyalgia. Front Pharmacol. 2011;2():17.
📝 需求与反馈
尽可能描述清楚需求与问题信息
