6-Desoxymorphine | 47024-28-2

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 吗啡烷
• 英文名称: 6-Desoxymorphine
• 英文别名: deoxymorphin-E；Desoxymorphin-E；(4R,4aR,7aS,12bS)-3-methyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-9-ol
• CAS: 47024-28-2
• 化学式: C₁₇H₁₉NO₂
• 分子量: 269.343
• InChiKey: JNJFKTKRRMLCEB-GMIGKAJZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  32.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-氯-1-苯基-1H-四唑 、 6-Desoxymorphine 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 以91.2%的产率得到(4R,4aR,7aS,12bS)-3-methyl-9-((1-phenyl-1H-tetrazol-5-yl)oxy)-2,3,4,4a,7,7a-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline
  参考文献：
  名称：

  Opioids and Efflux Transporters. Part 2: P-Glycoprotein Substrate Activity of 3- and 6-Substituted Morphine Analogs

  摘要：

  Continuing our studies investigating opioids with reduced P-glycoprotein (P-gp) substrate activity, a series of known 3- and 6-hydroxy, -methoxy, and -desoxymorphine analogs was synthesized and analyzed for Pgp substrate activity and opioid binding affinity. 6-Desoxymorphine (7) showed high affinity for opioid receptors and did not induce P-gp-mediated ATP hydrolysis. Additionally, 7 demonstrated morphine-like antinociceptive potency in mice, indicating this compound as an ideal lead to further evaluate the role of P-gp in opioid analgesic tolerance development.

  DOI：

  10.1021/jm701457j
• 作为产物：
  描述：

  3-甲氧基-4,5alpha-环氧-7,8-二去氢-17-甲基吗喃 在 三溴化硼 作用下， 以 氯仿 为溶剂， 反应 0.25h， 生成 6-Desoxymorphine
  参考文献：
  名称：

  Opioids and Efflux Transporters. Part 2: P-Glycoprotein Substrate Activity of 3- and 6-Substituted Morphine Analogs

  摘要：

  Continuing our studies investigating opioids with reduced P-glycoprotein (P-gp) substrate activity, a series of known 3- and 6-hydroxy, -methoxy, and -desoxymorphine analogs was synthesized and analyzed for Pgp substrate activity and opioid binding affinity. 6-Desoxymorphine (7) showed high affinity for opioid receptors and did not induce P-gp-mediated ATP hydrolysis. Additionally, 7 demonstrated morphine-like antinociceptive potency in mice, indicating this compound as an ideal lead to further evaluate the role of P-gp in opioid analgesic tolerance development.

  DOI：

  10.1021/jm701457j

文献信息

• Bone induction system and methods
  申请人：Vivex Biomedical Inc.

  公开号：US10434217B2

  公开（公告）日：2019-10-08

  An osteogenic composition suitable for use in bone and soft tissue reparative procedures is provided for herein. Methods for preparing osteogenic composition from blood and bone marrow are also provided for. The osteogenic compositions contain therapeutically effective concentrations of one or more osteogenic agents such as BMP-2, TGF-β, PDGF and VEGF.

  本文提供了一种适用于骨骼和软组织修复过程的成骨组合物。还提供了从血液和骨髓中制备成骨组合物的方法。成骨组合物含有治疗有效浓度的一种或多种成骨剂，如 BMP-2、TGF-β、PDGF 和 VEGF。
• Methods of producing nor-opioid and nal-opioid benzylisoquinoline alkaloids
  申请人：Antheia, Inc.

  公开号：US10738335B2

  公开（公告）日：2020-08-11

  A method of demethylizing an opioid to a nor-opioid is provided. The method comprises contacting an opioid with at least one enzyme. Contacting the opioid with the at least one enzyme converts the opioid to a nor-opioid. A method of converting a nor-opioid to a nal-opioid is provided. The method comprises contacting a nor-opioid with at least one enzyme. Contacting the nor-opioid with the at least one enzyme converts the nor-opioid to a nal-opioid.

  本发明提供了一种将阿片类药物去甲基化为非阿片类药物的方法。该方法包括将阿片类药物与至少一种酶接触。将阿片与至少一种酶接触可将阿片转化为去甲阿片。提供了一种将去甲阿片转化为正阿片的方法。该方法包括将去甲阿片与至少一种酶接触。将去甲阿片与至少一种酶接触可将去甲阿片转化为正阿片。
• Drug delivery composition
  申请人：——

  公开号：US20030170288A1

  公开（公告）日：2003-09-11

  The invention provides a drug delivery compositions and methods for treating pain. A drug delivery composition contains a polymer and at least two drugs sucha as an analgesic agent and an anesthetic agent.

  本发明提供了一种用于治疗疼痛的给药组合物和方法。一种给药组合物含有一种聚合物和至少两种药物，如镇痛剂和麻醉剂。
• Δ⁷-Desoxymorphine
  作者：Henry Rapoport、Robert M. Bonner

  DOI：10.1021/ja01155a552

  日期：1951.11
• METHODS FOR REGULATING NEUROTRANSMITTER SYSTEMS BY INDUCING COUNTERADAPTATIONS
  申请人：Michalow, Alexander

  公开号：EP2001495A2

  公开（公告）日：2008-12-17