麦角胺宁 | 639-81-6

• 物质功能分类: 有机原料 - 氨基化合物
• 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: 麦角胺宁
• 中文别名: 麦角异胺
• 英文名称: ergotaminine
• 英文别名: Isoergotamine；5'-benzyl-12'-hydroxy-2'-methyl-ergotamane-18,3',6'-trione；Ergotaminin；(5'α,8α)-12'-hydroxy-2'-methyl-5'-(phenylmethyl)-ergotaman-3',6',18-trione；Ergotamin；(6aR,9S)-N-[(1S,2S,4R,7S)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-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: 639-81-6
• 化学式: C₃₃H₃₅N₅O₅
• 分子量: 581.671
• InChiKey: XCGSFFUVFURLIX-BRMNWJGKSA-N

物化性质

• 熔点：
  252°C (rough estimate)
• 比旋光度：
  D20 +369° (c = 0.5 in chloroform)
• 沸点：
  639.99°C (rough estimate)
• 密度：
  1.2118 (rough estimate)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  43
• 可旋转键数：
  4
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  118
• 氢给体数：
  3
• 氢受体数：
  6

ADMET

毒理性

• 在妊娠和哺乳期间的影响

哺乳期使用总结：关于哺乳期间使用麦角胺的已发表经验有限，它可能会对婴儿产生不良影响并减少乳汁供应。大多数权威机构认为哺乳期间应禁忌使用麦角胺。 对哺乳婴儿的影响：一项研究中，将麦角胺在新生儿母亲分娩后立即以每天三次，每次1毫克，连续6天的剂量给药，发现对哺乳婴儿的体重增长没有影响。在母亲的乳汁完全下来之前的前几天，乳汁摄入量可能很少，因此婴儿的剂量可能很小。 对泌乳和母乳的影响：30名分娩足月婴儿的妇女在分娩后接受了单次肌内注射甲麦角新碱0.2毫克，随后口服麦角胺1毫克，每天三次，连续6天。与28名分娩足月婴儿且未接受任何麦角衍生物的妇女相比，两组在分娩后前6天的哺乳前后体重差异上没有区别，这表明乳汁产量没有差异。

◉ Summary of Use during Lactation:There is limited published experience with ergotamine during breastfeeding and it might cause adverse effects in the infant and decrease milk supply. Most authorities consider ergotamine to be contraindicated during nursing. ◉ Effects in Breastfed Infants:A study in which ergotamine was administered to mothers of newborns immediately postpartum in a dose of 1 mg 3 times daily for 6 days found no effect on weight gain in the breastfed infants. Milk intake, and therefore infant dosage, might have been minimal during the first few days before the mothers' milk came in fully. ◉ Effects on Lactation and Breastmilk:Thirty women who delivered fullterm infants received a single intramuscular dose of methylergonovine 0.2 mg after delivery, followed by oral ergotamine 1 mg 3 times daily for 6 days. Compared to 28 women who delivered fullterm infants and received no ergot derivatives, there was no difference in the milk production, as measured by weight differences before and after nursing, between the 2 groups during the first 6 days postpartum.

来源:Drugs and Lactation Database (LactMed)

安全信息

• 危险等级：
  6.1(b)
• 包装等级：
  III
• 危险类别：
  6.1(b)
• 危险品运输编号：
  UN 1544

反应信息

• 作为反应物：
  描述：

  麦角胺宁 、 甲烷磺酸 、 乙醚 以 乙醇 为溶剂， 以99.2% of the theory) with a melting point of 184°-187° C. was obtained的产率得到4-[[9,10-二氢-4-(甲基氨基)-9,10-二羰基蒽基]氨基]甲苯-3-磺化铵
  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
• 作为产物：
  描述：

  麦角胺 以 甲醇 为溶剂， 生成 麦角胺宁
  参考文献：
  名称：

  Bandula, Rodica; Vasilescu, Marilena, Revue Roumaine de Chimie, 1995, vol. 40, # 11-12, p. 1189 - 1196

  摘要：

  DOI：

文献信息

• Dialkylaminotetrahydroquinazoline
  申请人：ELI LILLY AND COMPANY

  公开号：EP0209983A1

  公开（公告）日：1987-01-28

  2-Permissibly- substituted-6- dialkylamino tetrahydroquinazolines, receptor agonists.

  2-Permissibly- substituted-6- dialkylamino tetrahydroquinazolines，受体激动剂。
• 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。
• DEGRADABLE SPIRAL COATED STENT WITH CONTROLLABLE GRADIENT, PREPARATION METHOD THEREFOR AND USE THEREOF
  申请人：Zhuhai Ruizhan Biomaterials Co., Ltd.

  公开号：EP3818995A1

  公开（公告）日：2021-05-12

  Disclosed are a spiral coated stent with controllable gradient degradation, a preparation method thereof and an application thereof. The spiral coated stent with controllable gradient degradation is composed of a degradable medical polyurethane and a degradable magnesium alloy material, wherein the degradable medical polyurethane contains a following chemical structure: PCL-PEG-PCL, wherein a molecular weight of the PEG is 200 to 1,000 and the molecular weight of the PCL is 200 to 10,000, and the degradable magnesium alloy material is of a spiral stent structure; and physical properties of the spiral coated stent with controllable gradient degradation need to satisfy the following technical parameters that: a breaking strength needs to be no less than 1 N, a pressure resistance needs to be no less than 2 N, and a degradation characteristic of the magnesium alloy after surface treatment shows gradient degradation with different time.

  本发明公开了一种可控梯度降解螺旋涂层支架、其制备方法及其应用。可控梯度降解螺旋涂层支架由可降解医用聚氨酯和可降解镁合金材料组成，其中可降解医用聚氨酯包含以下化学结构：PCL-PEG-PCL，其中PEG的分子量为200～1000，PCL的分子量为200～10000，可降解镁合金材料为螺旋支架结构；可控梯度降解螺旋涂层支架的物理性能需满足以下技术参数：断裂强度不小于1N，抗压强度不小于2N，镁合金表面处理后的降解特性随时间变化呈梯度降解。
• 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。