易咳嗪 | 10402-90-1

• 物质功能分类: 原料药 - 呼吸系统用药 - 镇咳药
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 易咳嗪
• 中文别名: 依普拉酮；1-(2-苯基-2-乙氧基)乙基-4-(2-苯甲酰基)丙基哌嗪；盐酸依普拉酮；双苯哌丙酮；苯丙哌酮
• 英文名称: eprazinone
• 英文别名: 1-(2-Ethoxy-2-phenylethyl)-4-(2-benzoylpropyl)piperazine；3-[4-(2-ethoxy-2-phenyl-ethyl)-piperazin-1-yl]-2-methyl-1-phenyl-propan-1-one；3-[4-(2-ethoxy-2-phenylethyl)piperazin-1-yl]-2-methyl-1-phenylpropan-1-one
• CAS: 10402-90-1
• 化学式: C₂₄H₃₂N₂O₂
• mdl: MFCD00866843
• 分子量: 380.53
• InChiKey: BSHWLCACYCVCJE-UHFFFAOYSA-N

物化性质

• 沸点：
  508.13°C (rough estimate)
• 密度：
  1.0909 (rough estimate)
• 熔点：
  160

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  28
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.458
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  4

安全信息

• 海关编码：
  2933599090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  室温

SDS

Material Safety Data Sheet

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Section 1. Identification of the substance
Product Name: Eprazinone
Synonyms:

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Section 2. Hazards identification
Harmful by inhalation, in contact with skin, and if swallowed.

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Section 3. Composition/information on ingredients.
Ingredient name: Eprazinone
CAS number: 10402-90-1

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Section 4. 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.

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Section 5. 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.

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Section 6. 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.

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Section 7. 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, refrigerated.
Storage:

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Section 8. 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.

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Section 9. Physical and chemical properties
Appearance: Not specified
Boiling point: No data
No data
Melting point:
Flash point: No data
Density: No data
Molecular formula: C24H32N2O2
Molecular weight: 380.5

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Section 10. Stability and reactivity
Conditions to avoid: Heat, flames and sparks.
Materials to avoid: Oxidizing agents.
Possible hazardous combustion products: Carbon monoxide, nitrogen oxides.

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Section 11. Toxicological information
No data.

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Section 12. Ecological information
No data.

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Section 13. 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.

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Section 14. Transportation information
Non-harzardous for air and ground transportation.

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Section 15. 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.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

药效学

苯丙哌酮是一种兼具中枢性和末梢性镇咳作用的非成瘾性药物，主要通过作用于咳嗽中枢来发挥效果。动物试验表明，它选择性地抑制脑干网状体，特别是延髓的咳嗽中枢。其作用强度与可待因相近或为其1/3，是美沙芬的2倍、那可丁的3倍。

临床研究表明，苯丙哌酮的镇咳效果与可待因相近或稍逊一筹，但不会引起如可待因那样对肠蠕动的抑制。此外，该药物还兼具祛痰作用，能够改变痰液中酸性糖蛋白的多糖纤维性质，使其粘多糖纤维膨胀断裂，从而具有较强的黏液溶解效果。实验还发现，苯丙哌酮还能发挥镇静、局麻及抗组胺、抗胆碱作用，缓解由组胺、乙酰胆碱和5-羟色胺引起的支气管平滑肌痉挛。

临床应用

依普拉酮主要用于治疗急性和慢性支气管炎、肺炎、哮喘以及肺结核等引起的咳嗽。尤其适用于慢性气管炎的镇咳祛痰。

用途

苯丙哌酮是一种用于急性和慢性支气管炎、肺炎、肺结核等多种疾病的镇咳祛痰药物，特别在治疗慢性气管炎方面表现突出。

反应信息

• 作为产物：
  描述：

  2-Ethoxy-2-phenylethan-1-amine 、 3-[bis(2-chloroethyl)amino]-2-methyl-1-phenylpropan-1-one 生成 易咳嗪
  参考文献：
  名称：

  MURAKAMI, YASUSI

  摘要：

  DOI：

文献信息

• SUBSTITUTED INDOLES
  申请人：Gant Thomas G.

  公开号：US20090191183A1

  公开（公告）日：2009-07-30

  Disclosed herein are substituted indole cysteinyl leukotriene receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

  本文揭示了Formula I的替代吲哚半胱氨酸白三烯受体调节剂，其制备方法，药物组合物以及使用方法。
• New CRTh2 antagonists
  申请人：Almirall, S.A.

  公开号：EP2548876A1

  公开（公告）日：2013-01-23

  The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.

  本发明涉及式(I)的化合物，制备这种化合物的方法以及它们在治疗病理状况或疾病中的应用，该病理状况或疾病容易通过CRTh2拮抗活性得到改善。
• [EN] COMPOUNDS AND COMPOSITIONS FOR OCULAR DELIVERY<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR ADMINISTRATION OCULAIRE
  申请人：GRAYBUG VISION INC

  公开号：WO2020069353A1

  公开（公告）日：2020-04-02

  The present invention provides new prodrags of Sunitinib, Brinzolamide, and Dorzolamide and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (TOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

  本发明提供了新的Sunitinib、Brinzolamide和Dorzolamide的前药，以及用于治疗医学疾病的组合物，例如青光眼、与眼内压增高有关的疾病或异常（TOP）、需要神经保护的疾病、年龄相关性黄斑变性或糖尿病视网膜病变。
• [EN] NEW CRTh2 ANTAGONISTS<br/>[FR] NOUVEAUX ANTAGONISTES DE CRTH2
  申请人：ALMIRALL SA

  公开号：WO2013010881A1

  公开（公告）日：2013-01-24

  The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.

  本发明涉及公式(I)的化合物，制备此类化合物的方法以及它们在治疗可通过CRTh2拮抗剂活性改善的病理状况或疾病中的用途。
• New bicyclic compounds as crac channel modulators
  申请人：Almirall, S.A.

  公开号：EP2738172A1

  公开（公告）日：2014-06-04

  The present invention relates to novel compounds which are inhibitors of CRAC channel activity. This invention also relates to pharmaceutical compositions containing them, process for their preparation and their use in therapy.

  这项发明涉及一种新型化合物，它们是CRAC通道活性的抑制剂。该发明还涉及含有这些化合物的药物组合物，它们的制备方法以及它们在治疗中的应用。