136236-51-6

• 常用中文名：雷沙吉兰
• 常用英文名：Rasagiline
• CAS号：136236-51-6
• 分子式：C₁₂H₁₃N
• 分子量：171.238
• 相关类别： 原料药 消化系统用药 食欲抑制药及其它减肥药
• 发布时间：2018-04-21 08:00:00
• 更新时间：2025-08-20 14:48:48
• 雷沙吉兰（AGN1135; TVP1012）是一种新的MAO-B抑制剂，用于治疗特发性帕金森病。靶：单胺氧化酶（MAO）-B雷沙吉兰（N-炔丙基-1-（R） - 氨基茚满）是一种新型，高效的不可逆单胺氧化酶（MAO）-B抑制剂，抗帕金森病药物。对于患有早期和晚期帕金森病（PD）的患者，雷沙吉兰可作为L-Dopa的单一疗法或辅助疗法。雷沙吉兰比司来吉兰更有效地抑制MAO-B，并且具有每日一次给药的优点。在一些大型，随机，安慰剂对照试验中，雷沙吉兰已证明在早期PD中作为单一疗法和在晚期PD中作为辅助疗法有效。此外，雷沙吉兰已被证明在体外和体内研究中具有神经保护作用。最近完成的延迟启动ADAGIO（疾病进展衰减，每日一次给予Azilect）试验表明，对于雷沙吉兰1 mg /天有潜在的疾病改善作用，尽管这一发现的临床意义尚未确定。已发现雷沙吉兰在早期PD的治疗中具有良好的耐受性和有效性，并且在运动波动中作为辅助治疗。拉沙吉兰是否与PD中临床上显着的神经保护（即疾病改变）相关是正在进行的临床试验的主题。

名称

• 中文名: 雷沙吉兰
• 英文名: Rasagiline
• 中文别名: (R)-2,3-二氢-N-2-丙烯基-1H-茚-1-胺; (R)-N-(2-丙炔基)-2,3-二氢茚-1-胺
• 英文别名: (1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine; (1R)-N-(Prop-2-yn-1-yl)indan-1-amine; (1R)-N-(2-Propyn-1-yl)-1-indanamine; (1R)-N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine; Rasagiline; (1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine; (R)-N-(2-Propynyl)-2,3-dihydroinden-1-amine

物化性质

• 密度: 1.1±0.1 g/cm3
• 沸点: 305.5±30.0 °C at 760 mmHg
• 熔点: 35-41°C
• 分子式: C₁₂H₁₃N
• 分子量: 171.238
• 闪点: 146.8±20.0 °C
• 精确质量: 171.104797
• PSA: 12.03000
• LogP: 2.27
• 蒸汽压: 0.0±0.6 mmHg at 25°C
• 折射率: 1.577
• 储存条件: 2-8°C

生物活性

• 描述: Rasagiline(AGN1135;TVP1012)是MAO-B抑制剂,可作用于原发性帕金森病。
• 相关类别:
  信号通路 >> 神经信号通路 >> 单胺氧化酶
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Leegwater-Kim, J. and E. Bortan, The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging, 2010. 5: p. 149-56.

  [2]. Weinreb, O., et al., Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol, 2010. 92(3): p. 330-44.

  [3]. Chen, J.J., D.M. Swope, and K. Dashtipour, Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther, 2007. 29(9): p. 1825-49.

MSDS

Material Safety Data Sheet Section1. Identification of the substance Product Name: Rasagiline Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Rasagiline CAS number:136236-51-6 Section4. First aid measures Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing contaminated clothing and shoes. If irritation persists, seek medical attention. Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical attention. Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention. Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention. Section5. Fire fighting measures In the event of a fire involving this material, alone or in combination with other materials, use dry powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus should be worn. Section6. Accidental release measures Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national standards. Respiratory precaution:Wear approved mask/respirator Hand precaution:Wear suitable gloves/gauntlets Skin protection:Wear suitable protective clothing Eye protection:Wear suitable eye protection Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container for disposal. See section 12. Environmental precautions: Do not allow material to enter drains or water courses. Section7. Handling and storage Handling:This product should be handled only by, or under the close supervision of, those properly qualified in the handling and use of potentially hazardous chemicals, who should take into account the fire, health and chemical hazard data given on this sheet. Store in closed vessels. Storage: Section8. Exposure Controls / Personal protection Engineering Controls: Use only in a chemical fume hood. Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles. General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse. Section9. Physical and chemical properties Appearance:Not specified Boiling point:No data No data Melting point: Flash point:No data Density:No data Molecular formula:C12H13N Molecular weight:171.2 Section10. Stability and reactivity Conditions to avoid: Heat, flames and sparks. Materials to avoid: Oxidizing agents. Possible hazardous combustion products: Carbon monoxide, nitrogen oxides. Section11. Toxicological information No data. Section12. Ecological information No data. Section13. Disposal consideration Arrange disposal as special waste, by licensed disposal company, in consultation with local waste disposal authority, in accordance with national and regional regulations. Section14. Transportation information Non-harzardous for air and ground transportation. Section15. Regulatory information No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302, or have known CAS numbers that exceed the threshold reporting levels established by SARA Title III, Section 313. SECTION 16 - ADDITIONAL INFORMATION N/A

安全

• 危害码 (欧洲): Xi
• 海关编码: 2921499090

合成路线

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海关

海关编码	2921499090
中文概述	2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无 最惠国关税:6.5% 普通关税:30.0%
申报要素	品名, 成分含量, 用途
Summary	2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%