80012-43-7

• 常用中文名：依匹斯汀
• 常用英文名：Epinastine
• CAS号：80012-43-7
• 分子式：C₁₆H₁₅N₃
• 分子量：249.31000
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-07-11 16:11:39
• 更新时间：2024-01-04 18:23:07
• Epinastine(WAL801)是抗组胺和肥大细胞稳定剂,可作用于过敏性结膜炎。

名称

• 中文名: 依匹斯汀
• 英文名: epinastine
• 中文别名: 3-氨基-9,13-二氢-1H-二苯并[c,f]咪唑并[1,5-a]氮杂卓
• 英文别名: EPINASTINE BASE; 9,13b-Dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepin-3-amine; Flurinol(R); 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine; Epinastine; 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine; MFCD00865648

物化性质

• 密度: 1.32 g/cm3
• 沸点: 428ºC at 760 mmHg
• 熔点: 270ºC
• 分子式: C₁₆H₁₅N₃
• 分子量: 249.31000
• 闪点: 212.7ºC
• 精确质量: 249.12700
• PSA: 41.62000
• LogP: 2.66770
• 外观性状: 白色至黄色结晶粉末
• 折射率: 1.727
• 储存条件: 2-8℃

生物活性

• 描述: Epinastine(WAL801)是抗组胺和肥大细胞稳定剂,可作用于过敏性结膜炎。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. Fugner, A., et al., In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung, 1988. 38(10): p. 1446-53.

  [2]. Roeder, T., J. Degen, and M. Gewecke, Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol, 1998. 349(2-3): p. 171-7.

  [3]. Kamei, C., et al., Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol, 1992. 14(1-2): p. 191-205.

  [4]. Kohyama, T., et al., A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun, 1997. 230(1): p. 125-8.

MSDS

Material Safety Data Sheet Section1. Identification of the substance Product Name: Epinastine Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Epinastine CAS number:80012-43-7 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:C16H15N3 Molecular weight:249.3 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

合成路线

127786-29-2 ~93% 80012-43-7

文献：USV LIMITED Patent: WO2009/63504 A2, 2009 ; Location in patent: Page/Page column 25 ;

127785-96-0 ~% 80012-43-7

文献：WO2009/63504 A2, ; Page/Page column 24 ;

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