Nasalide

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: Nasalide
• 英文别名: 19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one
• 化学式: C₂₄H₃₁FO₆
• 分子量: 434.5
• InChiKey: XSFJVAJPIHIPKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  31
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  93.1
• 氢给体数：
  2
• 氢受体数：
  7

ADMET

毒理性

• 在妊娠和哺乳期间的影响

使用说明: 尽管没有测量，但吸入皮质类固醇进入母体血液和排入母乳的量可能太小，不会影响哺乳婴儿。审阅者和专家小组认为，在哺乳期间可以使用吸入和口服皮质类固醇。 对哺乳婴儿的影响: 截至修订日期，没有发现任何皮质类固醇对哺乳婴儿有影响。 对泌乳和母乳的影响: 截至修订日期，没有找到相关的已发布信息。

◉ Summary of Use during Lactation:Although not measured, the amounts of inhaled corticosteroids absorbed into the maternal bloodstream and excreted into breastmilk are probably too small to affect a breastfed infant. Reviewers and an expert panel consider inhaled and oral corticosteroids acceptable to use during breastfeeding. ◉ Effects in Breastfed Infants:None reported with any corticosteroid. ◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.

来源:Drugs and Lactation Database (LactMed)

文献信息

• CORTICOSTEROID CONJUGATES AND USES THEREOF
  申请人：Teicher Martin H.

  公开号：US20100056488A1

  公开（公告）日：2010-03-04

  The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.
• Oligomer-Corticosteroid Conjugates
  申请人：Zhang Wen

  公开号：US20100286107A1

  公开（公告）日：2010-11-11

  The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
• OLIGOMER-CORTICOSTEROID CONJUGATES
  申请人：NAKTAR THERAPEUTICS

  公开号：US20140309398A1

  公开（公告）日：2014-10-16

  The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits different properties compared to the properties of the corticosteroid not attached to the water-soluble oligomer.
• US8796248B2
  申请人：——

  公开号：US8796248B2

  公开（公告）日：2014-08-05
• [EN] OLIGOMER-CORTICOSTEROID CONJUGATES<br/>[FR] CONJUGUÉS D'OLIGOMÈRES ET CORTICOSTÉROÏDES
  申请人：NEKTAR THERAPEUTICS AL CORP

  公开号：WO2009045539A2

  公开（公告）日：2009-04-09

  The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.