[8β(1S，2R)]-N-(2-羟基环戊基)-6-甲基-1-(1-甲基乙基)-麦角灵-8-羧酰胺 | 137328-52-0

• 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: [8β(1S，2R)]-N-(2-羟基环戊基)-6-甲基-1-(1-甲基乙基)-麦角灵-8-羧酰胺
• 英文名称: LY 215840
• 英文别名: (6aR,9R,10aR)-N-[(1S,2R)-2-hydroxycyclopentyl]-7-methyl-4-propan-2-yl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-9-carboxamide
• CAS: 137328-52-0
• 化学式: C₂₄H₃₃N₃O₂
• 分子量: 395.5
• InChiKey: IMSDOBUYDTVEHN-ILMFXRJHSA-N

物化性质

• 沸点：
  642.1±55.0 °C(Predicted)
• 密度：
  1.34±0.1 g/cm3(Predicted)
• 溶解度：
  在 DMSO 中溶解度为 100 mM，在乙醇中溶解度为 25 mM

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  57.5
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Systems pharmacology for treating ocular disorders
  申请人：Case Western Reserve University

  公开号：US10117868B2

  公开（公告）日：2018-11-06

  A method of treating an ocular disorder in a subject includes administering to the subject subtherapeutic amounts of two or more agents that inhibit and/or blocks the activation of Gs- or Gq-protein coupled receptors or Gs- or Gq-signaling cascade in ocular cells of the subject, and/or activates Gi-protein coupled receptors, which is induced or triggered by light induced all-trans-retinal generation.

  一种治疗受试者眼部疾病的方法包括向受试者施用亚治疗量的两种或两种以上抑制和/或阻断受试者眼部细胞中 Gs 或 Gq 蛋白偶联受体或 Gs 或 Gq 信号级联激活的制剂，和/或激活 Gi- 蛋白偶联受体，这是由光诱导全反式视网膜生成诱导或触发的。
• Compositions and methods of treating diabetic retinopathy
  申请人：CASE WESTERN RESERVE UNIVERSITY

  公开号：US10272106B2

  公开（公告）日：2019-04-30

  A method of treating diabetic retinopathy in a subject in need thereof includes administering to the subject a therapeutically effective amount of one or more agents that act as a trap of reactive aldehydes and/or inhibit diabetes-induced superoxide generation and capillary degeneration regulated by GPCR signaling pathways.

  一种治疗糖尿病视网膜病变受试者的方法包括向受试者施用一种或多种治疗有效量的制剂，这些制剂可作为活性醛的捕获剂和/或抑制糖尿病诱导的超氧化物生成和由 GPCR 信号通路调节的毛细血管变性。
• Compounds and methods of treating ocular disorders
  申请人：Case Western Reserve University

  公开号：US10568851B2

  公开（公告）日：2020-02-25

  A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).

  一种治疗受试者眼部疾病的方法包括向受试者施用治疗有效量的制剂，该制剂可调节与光诱导视网膜变性、全反式视网膜异常积聚和/或活性氧（ROS）生成相关的信号级联中的至少一个靶点。
• COMPOUNDS AND METHODS OF TREATING OCULAR DISORDERS
  申请人：Case Western Reserve University

  公开号：US20140235562A1

  公开（公告）日：2014-08-21

  A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).
• TWO-PHOTON MICROSCOPY IMAGING RETINA CELL DAMAGE
  申请人：POLGENIX, INC.

  公开号：US20160345827A1

  公开（公告）日：2016-12-01

  A method of determining retinal degeneration of photoreceptors and/or the retinal pigment epithelium (RPE) of a subject includes measuring two-photon induced fluorescence inner and/or outer segments of the photoreceptor cells and/or retinal pigment epithelium to assess photoreceptor cell death and retinal pigment epithelium cell death or degeneration.