麦角异克碱 | 511-07-9

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 麦角林及其衍生物
• 中文名称: 麦角异克碱
• 中文别名: 异麦角克碱
• 英文名称: Ergocristinine
• 英文别名: (6aR,9S)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-5,8-dioxo-4-propan-2-yl-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinoline-9-carboxamide
• CAS: 511-07-9
• 化学式: C₃₅H₃₉N₅O₅
• 分子量: 609.7
• InChiKey: HEFIYUQVAZFDEE-NASJTFDLSA-N

物化性质

• 熔点：
  226℃ (decomposition) (ethanol )
• 比旋光度：
  D20 +366° (c = 0.68 in chloroform); +471° (c = 0.35 in pyridine)
• 沸点：
  655.69°C (rough estimate)
• 密度：
  1.1839 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  45
• 可旋转键数：
  5
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  118
• 氢给体数：
  3
• 氢受体数：
  6

安全信息

• 危险等级：
  6.1(b)
• 包装等级：
  III
• 危险类别：
  6.1(b)

反应信息

• 作为反应物：
  描述：

  麦角异克碱 、 甲烷磺酸 、 乙醚 以 乙醇 为溶剂， 以96.4% of the theory) with a melting point of 170°-180° C. was obtained的产率得到Ergocristinine methanesulfonate
  参考文献：
  名称：

  Acid addition salts of dextrorotatory ergot alkaloids, a process for the

  摘要：

  含有麦角胺盐、麦角肽、麦角隐肽、麦角晶肽和麦角糠肽的药物，用于治疗动脉高血压、心力衰竭、心律不齐或头痛。

  公开号：

  US04440772A1

文献信息

• Methods for making sustained-release pharmaceutical compositions of ergot alkaloids having improved bioavailability and compositions thereof
  申请人：Polichem S.A.

  公开号：EP1512403A1

  公开（公告）日：2005-03-09

  A method of improving bioavailability of ergot derivatives administered using sustained-release delivery systems includes combining an ergot derivative or mixture thereof with a pharmaceutically acceptable hydrophilic swelling agent or mixture thereof and one or more pharmaceutically acceptable excipients. The bioavailability of sustained-release formulations of the present invention is at least equal to the bioavailability of the ergot derivative or mixture thereof administered using a conventional delivery system. Sustained-release compositions that improve bioavailability are also provided. Methods and compositions according to the present invention may provide sustained-release characteristics while improving the bioavailability of ergot derivatives.

  一种利用缓释给药系统提高麦角衍生物生物利用度的方法包括将麦角衍生物或其混合物与药学上可接受的亲水性膨胀剂或其混合物以及一种或多种药学上可接受的赋形剂相结合。本发明缓释制剂的生物利用度至少等于使用传统给药系统给药的麦角衍生物或其混合物的生物利用度。本发明还提供了可提高生物利用度的缓释组合物。根据本发明的方法和组合物可以提供缓释特性，同时提高麦角衍生物的生物利用度。
• Improved protein production
  申请人：Boehringer Ingelheim RCV GmbH & Co KG

  公开号：EP2952584A1

  公开（公告）日：2015-12-09

  The present invention is in the field of recombinant biotechnology, in particular in the field of protein expression. The invention generally relates to a method of expressing a protein of interest (POI) from a host cell by overexpressing a polynucleotide encoding a protein which is involved in one or more proteinogenic amino acid biosynthesis pathways, thereby increasing the yield of a protein of interest. The invention relates particularly to improving a host cell's capacity to express and/or secrete a protein of interest and use of the host cell for protein expression. The invention also relates to cell culture technology, and more specifically to culturing cells to produce desired molecules for medical purposes or food products.

  本发明属于重组生物技术领域，特别是蛋白质表达领域。本发明一般涉及一种通过过表达编码参与一种或多种蛋白质氨基酸生物合成途径的蛋白质的多核苷酸，从宿主细胞中表达感兴趣的蛋白质（POI），从而提高感兴趣的蛋白质产量的方法。本发明尤其涉及提高宿主细胞表达和/或分泌相关蛋白质的能力，以及利用宿主细胞表达蛋白质。本发明还涉及细胞培养技术，更具体地说，涉及培养细胞以生产用于医疗目的或食品的所需分子。
• Improved protein production in fungi or yeasts
  申请人：Boehringer Ingelheim RCV GmbH & Co KG

  公开号：EP2952585A1

  公开（公告）日：2015-12-09

  The present invention is in the field of recombinant biotechnology, in particular in the field of protein expression. The invention generally relates to a method of expressing a protein of interest (POI) from a host cell by overexpressing a polynucleotide encoding a protein which is involved in one or more proteinogenic amino acid biosynthesis pathways, thereby increasing the yield of a protein of interest. The invention relates particularly to improving a host cell's capacity to express and/or secrete a protein of interest and use of the host cell for protein expression. The invention also relates to cell culture technology, and more specifically to culturing cells to produce desired molecules for medical purposes or food products.

  本发明属于重组生物技术领域，特别是蛋白质表达领域。本发明一般涉及一种通过过表达编码参与一种或多种蛋白质氨基酸生物合成途径的蛋白质的多核苷酸，从宿主细胞中表达感兴趣的蛋白质（POI），从而提高感兴趣的蛋白质产量的方法。本发明尤其涉及提高宿主细胞表达和/或分泌相关蛋白质的能力，以及利用宿主细胞表达蛋白质。本发明还涉及细胞培养技术，更具体地说，涉及培养细胞以生产用于医疗目的或食品的所需分子。
• Topical regional neuro-affective therapy with cannabinoid combination products
  申请人：Afgin Pharma, LLC

  公开号：US10383816B2

  公开（公告）日：2019-08-20

  A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a cannabinoid drug(s) and a second therapeutically active agent(s) to the back of the neck of a human patient to provide regional neuro-affective therapy is disclosed. In certain preferred embodiments, the cannabinoid drug(s) are not psychoactive or substantially not psychoactive. In certain embodiments, the drugs are incorporated into a pharmaceutically acceptable topical carrier, e.g., a cream. In certain preferred embodiments, the cannabinoid drug(s) comprises cannabidiol.

  本发明公开了一种通过局部脑干传入刺激疗法治疗人类疾病状态或病症的方法，该方法是在人类患者的后颈部施用一种（多种）大麻素药物和第二种（多种）治疗活性剂，以提供区域神经情感疗法。在某些优选的实施方案中，大麻素药物不具有精神活性或基本上不具有精神活性。在某些实施方案中，药物被掺入药学上可接受的局部载体中，如乳膏。在某些优选的实施方案中，大麻素药物包括大麻二酚。
• Recombinant host cell for expressing proteins of interest
  申请人：Boehringer Ingelheim RCV GmbH & Co KG

  公开号：US10590427B2

  公开（公告）日：2020-03-17

  The present invention is in the field of recombinant biotechnology, in particular in the field of protein expression. The invention generally relates to a method of expressing a protein of interest (POI) from a host cell. The invention relates particularly to improving a host cell's capacity to express and/or secrete a protein of interest and use of the host cell for protein expression. The invention also relates to cell culture technology, and more specifically to culturing cells to produce desired molecules for medical purposes or food products.

  本发明属于重组生物技术领域，特别是蛋白质表达领域。本发明一般涉及一种从宿主细胞表达感兴趣的蛋白质（POI）的方法。本发明尤其涉及提高宿主细胞表达和/或分泌感兴趣蛋白质的能力，以及使用宿主细胞表达蛋白质。本发明还涉及细胞培养技术，更具体地说，涉及培养细胞以生产用于医疗目的或食品的所需分子。