17-羟基孕甾-4-烯-3-酮 | 1235-97-8

• 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
• 中文名称: 17-羟基孕甾-4-烯-3-酮
• 英文名称: 17α-ethylandrost-4-en-17β-ol-3-one
• 英文别名: 17-hydroxy-17βH-pregn-4-en-3-one；17-Hydroxy-17βH-pregn-4-en-3-on；17-Hydroxy-17βH-pregnen-(4)-on-(3)；norethandrolone；Ethyltestosterone；(8R,9S,10R,13S,14S,17S)-17-ethyl-17-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-one
• CAS: 1235-97-8
• 化学式: C₂₁H₃₂O₂
• 分子量: 316.484
• InChiKey: FGPGANCDNDLUST-CEGNMAFCSA-N

物化性质

• 溶解度：
  可溶于氯仿（少许）、甲醇（少许）
• 物理描述：
  Solid

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  23
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  17-羟基孕甾-4-烯-3-酮 生成 Δ^4.17-Pregnadienon-(3)
  参考文献：
  名称：

  藻红蛋白。细胞摄取和定位，光敏化和光谱评估的机理。

  摘要：

  目的通过研究叶绿素的细胞吸收和细胞内定位模式及其在中国仓鼠肺成纤维细胞（V79）中的光谱特性，阐明叶绿素的光生物学行为。方法将菊红素稀释在二甲基亚砜（DMSO）中。使用配备有红敏光电倍增管的发光光谱仪测量荧光发射光谱和激发光谱。将V79细胞单层培养，并用0.25 microg / ml叶绿素标记，以用于摄取，细胞存活和细胞内定位研究。为了进行细胞存活和细胞内定位研究，随后将细胞以9.0 mW / cm2的通量率暴露于蓝光下。结果叶绿素在DMSO中的荧光激发光谱的特征是Soret谱带在418 nm处有最大峰。荧光发射光谱在643和706nm处具有峰。细胞中相应的光谱分别红移至422、650和712 nm。温育约10小时后，叶绿素的细胞吸收完成。摄取，活化能以及使用叶绿素在37摄氏度和0摄氏度下使用荧光显微镜观察的细胞分析表明，染料是通过扩散介导的途径吸收到细胞中的。叶绿素处理过的细胞曝光后，

  DOI：

  10.1080/00480169.2002.36291
• 作为产物：
  描述：

  去氢表雄酮 在 jones reagent 作用下， 以 四氢呋喃 、 丙酮 为溶剂， 反应 0.08h， 生成 17-羟基孕甾-4-烯-3-酮
  参考文献：
  名称：

  Giacopello, Sergio; Deluca, Monica E.; Seldes, Alicia M., Zeitschrift fur Naturforschung, B: Chemical Sciences, 1992, vol. 47, # 6, p. 891 - 897

  摘要：

  DOI：

文献信息

• Porous drug matrices and methods of manufacture thereof
  申请人：Acusphere Inc.

  公开号：US20020142050A1

  公开（公告）日：2002-10-03

  Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

  药物，特别是低水溶性药物，以多孔性矩阵形式提供，最好是微粒，这可以增强药物在水性介质中的溶解。药物矩阵最好是使用包括以下步骤的过程制备的：(i)将药物，最好是低水溶性药物，溶解在挥发性溶剂中形成药物溶液，(ii)将至少一种孔形成剂与药物溶液结合形成乳液、悬浮液或第二溶液和亲水或疏水的赋形剂，以稳定药物并抑制结晶，(iii)从乳液、悬浮液或第二溶液中除去挥发性溶剂和孔形成剂，以得到多孔性的药物矩阵。亲水或疏水的赋形剂可以被选择用于通过抑制晶体生长来稳定药物的晶体形式，或者用于通过防止结晶来稳定药物的非晶形式。孔形成剂可以是与药物溶剂不相溶的挥发性液体或挥发性固体化合物，最好是挥发性盐。在一个优选实施例中，喷雾干燥用于除去溶剂和孔形成剂。所得到的多孔性矩阵在给患者治疗后具有更快的溶解速率，与非多孔性药物矩阵形式相比。在一个优选实施例中，多孔性药物矩阵的微粒被重组与水性介质，并通过标准技术处理成口服片剂或胶囊剂进行口服给药。
• Microbial transformation of 17α-ethynyl- and 17α-ethylsteroids, and tyrosinase inhibitory activity of transformed products
  作者：M CHOUDHARY、S SULTAN、M KHAN、A RAHMAN

  DOI：10.1016/j.steroids.2005.05.002

  日期：2005.11

  microbial transformation of the 17alpha-ethynyl-17beta-hydroxyandrost-4-en-3-one (1) (ethisterone) and 17alpha-ethyl-17beta-hydroxyandrost-4-en-3-one (2) by the fungi Cephalosporium aphidicola and Cunninghamella elegans were investigated. Incubation of compound 1 with C. aphidicola afforded oxidized derivative, 17alpha-ethynyl-17beta-hydroxyandrosta-1,4-dien-3-one (3), while with C. elegans afforded

  蚜虫头孢霉菌对17alpha-乙炔基17beta-羟基雄蕊-4-en-3-one（1）和17alpha-乙基-17beta-羟基雄蕊-4-en-3-one（2）的微生物转化和秀丽线虫进行了调查。将化合物1与蚜虫C.一起孵育可得到氧化的衍生物17α-乙炔基17β-羟基androsta-1,4-dien-3-one（3），而秀丽隐杆线虫则提供了一种新的羟基衍生物17α-乙炔基11alpha， 17beta-dihydroxyandrost-4-en-3-one（4）。另一方面，将化合物2与蚜虫C.aphidicola一起温育，得到17α-乙基-17β-羟基雄甾烯-1,4-二烯-3-酮（5）。两种新的羟基衍生物，17alpha-ethyl-11alpha，17beta-dihydroxyandrost-4-en-3-one（6）和17alpha-ethyl-6alpha，17beta-dihyd
• [EN] TOPICAL FORMULATIONS BASED ON IONIC SPECIES FOR SKIN TREATMENT<br/>[FR] FORMULATIONS TOPIQUES A BASE D'ESPÈCES IONIQUES POUR LE TRAITEMENT DE LA PEAU
  申请人：UNIV CALIFORNIA

  公开号：WO2018044920A1

  公开（公告）日：2018-03-08

  Compositions containing a complex that contains a cation with alkyl chains and a macromolecule anion, and methods of making and using are disclosed. The compositions are typically charge neutral and a liquid at room temperature and standard pressure. The macromolecule anions may be nucleic acids, peptides, proteins, and/or carbohydrates. The compositions have enhanced penetration across the skin barrier (stratum corneum) and into the skin cells, delivering the macromolecules to the skin cells. The compositions are topically applied to the skin and are particularly useful for treatment of skin conditions.

  本发明揭示了含有含有烷基链阳离子和大分子阴离子的复合物的组合物及其制备和使用方法。这些组合物通常是电中性的，且在常温和标准压力下呈液态。大分子阴离子可以是核酸、肽、蛋白质和/或碳水化合物。这些组合物可以增强穿透皮肤屏障（角质层）并进入皮肤细胞，将大分子输送到皮肤细胞中。这些组合物可局部应用于皮肤，尤其适用于治疗皮肤状况。
• Sustained release pharmaceutical formulation for inhalation
  申请人：——

  公开号：US20040105821A1

  公开（公告）日：2004-06-03

  Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to the lungs of a patient by inhalation. The formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon inhalation of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles in the lungs for at least 2 hours. Preferably, a majority of the pharmaceutical agent is released from the microparticles by 24 hours following inhalation, for example where a majority of the pharmaceutical agent is released no earlier than about 2 hours and no later than about 24 hours following inhalation. Methods for delivering a pharmaceutical agent, such as a corticosteroid, to the lungs of a patient are also provided. For example, the method includes having the patient inhale a dry powder blend comprising the present microparticles and a pharmaceutically acceptable bulking agent.

  提供了一种药物制剂和方法，通过吸入将药物剂量持续释放到患者的肺部。该制剂包括多孔微粒，其中包括药物剂量和基质材料，吸入该制剂后，肺部至少释放出治疗或预防有效剂量的药物剂量，持续时间至少为2小时。最好，药物剂量的大部分在吸入后的24小时内从微粒中释放出来，例如，药物剂量的大部分在吸入后不早于约2小时，不晚于约24小时内释放。还提供了将药物剂量（例如皮质类固醇）传递到患者肺部的方法。例如，该方法包括让患者吸入包括当前微粒和药用可接受的增容剂的干粉混合物。
• Injectable, oral, or topical sustained release pharmaceutical formulations
  申请人：Bernstein Howard

  公开号：US20050069591A1

  公开（公告）日：2005-03-31

  Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to a patient by injection, by oral administration or by topical administration. The injectable formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon injection of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 24 hours. The oral formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 2 hours following oral administration. The topical formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles for at least 2 hours following topical administration.

  提供了药物制剂和方法，通过注射、口服或局部给药使药物代理持续释放给患者。可注射的制剂包括多孔微粒，其包括药物代理和基质材料，在注射制剂后，药物代理的治疗或预防有效量将从微粒中释放至少24小时。口服制剂包括多孔微粒，其包括药物代理和基质材料，在口服后，药物代理的治疗或预防有效量将从微粒中释放至少2小时。局部制剂包括多孔微粒，其包括药物代理和基质材料，在局部给药后，药物代理的治疗或预防有效量将从微粒中释放至少2小时。