testosterone 17β-N,N-dimethylglycinate

• 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: testosterone 17β-N,N-dimethylglycinate
• 英文别名: [(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 2-(dimethylamino)acetate
• 化学式: C₂₃H₃₅NO₃
• 分子量: 373.536
• InChiKey: KLLMZSGJZUFEJU-WAUHAFJUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  睾酮 、 (二甲基氨基)乙酰氯 在 盐酸 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 testosterone 17β-N,N-dimethylglycinate
  参考文献：
  名称：

  睾丸激素17beta-N，N-N-二甲基甘氨酸盐酸盐：一种前体药物，可能通过鼻腔递送睾丸激素。

  摘要：

  这项研究的目的是研究使用水溶性前药TS17β-N，N-二甲基甘氨酸盐酸盐对难溶性药物睾丸激素（TS）进行全身给药的鼻腔途径。在大鼠中进行了前药的理化性质，人肝匀浆的体外水解以及体内鼻腔和静脉内实验。前体药物的水溶解度大于100 mg / mL，而TS的水溶解度为0.01 mg / mL，其在0.05 M，磷酸盐缓冲液（pH 6）和辛醇之间的对数分配系数为2.4。发现该前药在33％的人肝匀浆中产生TS，并迅速而定量地从鼻腔吸收。经鼻给药前药后，前药和TS的生物利用度均与等效静脉内给药后相似。这些在大鼠中的研究表明，TS的这种水溶性前药可能具有治疗TS缺乏症的治疗作用。

  DOI：

  10.1002/jps.10083

文献信息

• Controlled release delivery system for nasal applications
  申请人：Mattern Claudia

  公开号：US20050100564A1

  公开（公告）日：2005-05-12

  This invention relates to a pernasally administrable preparation for the controlled release of sexual hormones to the systemic circulation, in particular to a formulation which enables its active ingredient to be absorbed in a sustained manner providing a better bioavailability at very low doses and longer duration of action.

  本发明涉及一种可经鼻腔给药的制剂，用于将性激素控制释放到全身循环中，特别是涉及一种制剂，这种制剂能使其活性成分以持续的方式被吸收，从而在极低剂量时具有更好的生物利用率和更长的作用时间。
• Controlled release delivery system of sexual hormones for nasal application
  申请人：Mattern, Udo

  公开号：EP1530965B1

  公开（公告）日：2006-03-08
• CONTROLLED RELEASE NASAL TESTOSTERONE GELS, METHODS AND PRE-FILLED MULTI-DOSE APPLICATOR SYSTEMS FOR PERNASAL ADMINISTRATION
  申请人：Trimel Biopharma SRL

  公开号：EP2709588A1

  公开（公告）日：2014-03-26
• Controlled Release Delivery System for Nasal Applications and Method of Treatment
  申请人：MATTERN Claudia

  公开号：US20070149454A1

  公开（公告）日：2007-06-28

  This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and/or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.
• CONTROLLED RELEASE DELIVERY SYSTEM FOR NASAL APPLICATIONS AND METHODS OF TREATMENT
  申请人：MATTERN Claudia

  公开号：US20100311707A1

  公开（公告）日：2010-12-09

  This invention relates to a gel formulation for nasal administration of a controlled release formulation of hormones to the systemic circulation and/or to the brain. The special lipophilic or partly lipophilic system of the invention leads to higher bioavailability of the active ingredient caused by sustained serum levels in plasma but also leads to a more favorable serum level profile. The special lipophilic or partly lipophilic system also allows for the modulation of brain functioning. The invention also relates to the nasal administration of steroid hormones for treatment of female sexual dysfunction (FSD) or female arousal disorder.