(S)-2-Methyl-butyric acid (1S,3R,7S,8S,8aR)-8-[2-((R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydro-naphthalen-1-yl ester

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酯类
• 英文名称: (S)-2-Methyl-butyric acid (1S,3R,7S,8S,8aR)-8-[2-((R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydro-naphthalen-1-yl ester
• 英文别名: [(1S,3R,7S,8S,8aR)-8-[2-[(4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate
• 化学式: C₂₄H₃₆O₅
• 分子量: 404.5
• InChiKey: PCZOHLXUXFIOCF-KVVRZSONSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  72.8
• 氢给体数：
  1
• 氢受体数：
  5

ADMET

毒理性

• 在妊娠和哺乳期间的影响

母乳喂养期间使用概述：目前没有关于在母乳喂养期间使用洛伐他汀的相关已发表信息。由于担心会干扰婴儿的脂质代谢，共识认为在母乳喂养期间不应使用洛伐他汀。然而，也有人认为，对于家族性高胆固醇血症的纯合子儿童，从1岁开始就使用他汀类药物，他汀类药物的口服生物利用度较低，对哺乳婴儿的风险较低，尤其是瑞舒伐他汀和阿托伐他汀。[1]在更多数据可用之前，可能首选另一种药物，特别是在哺乳新生儿或早产儿时。 对哺乳婴儿的影响：截至修订日期，未找到相关已发表信息。 对泌乳和母乳的影响：截至修订日期，未找到相关已发表信息。

◉ Summary of Use during Lactation:No relevant published information exists on the use of lovastatin during breastfeeding. Because of a concern with disruption of infant lipid metabolism, the consensus is that lovastatin should not be used during breastfeeding. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin.[1] Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ 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

• LOVASTATIN ESTERASE ENZYME IMMOBILIZED ON SOLID SUPPORT, PROCESS FOR ENZYME IMMOBILIZATION, BIOCATALYTIC FLOW REACTOR AND PROCESS FOR PREPARATION AND/OR PURIFICATION OF SIMVASTATIN
  申请人：Instytut Chemii Organicznej, Polska Akademia Nauk

  公开号：EP2240569B1

  公开（公告）日：2013-09-11
• PREPARATION AND UTILITY OF HMG-COA REDUCTASE INHIBITORS
  申请人：Gant Thomas G.

  公开号：US20100137244A1

  公开（公告）日：2010-06-03

  Chemical syntheses and medical uses of novel modulators of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and diastereomeric mixtures of isomers, individual diastereomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of hypercholesterolemia, dyslipidemia, coronary artery disease, atherosclerosis, metabolic syndrome, a hyperproliferative disease such as colorectal cancer, prostate cancer, and melanoma, a neurodegenerative disease such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease are described.
• LOCAL COCHLEAR APPLICATION OF STATINS FOR STIMULATING NEURITE REGROWTH IN THE COCHLEA
  申请人：Whitlon Donna S.

  公开号：US20140179723A1

  公开（公告）日：2014-06-26

  Statin compositions are disclosed for stimulating neurite growth from spiral ganglion neurons in the inner ear and methods for preventing damage to or treating damage of auditory neurons and/or hair cells of the cochlea following acoustic or toxic insult.
• US7407772B2
  申请人：——

  公开号：US7407772B2

  公开（公告）日：2008-08-05
• US7566792B2
  申请人：——

  公开号：US7566792B2

  公开（公告）日：2009-07-28