盐酸咪奈丁 | 30272-08-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 二苯并环庚烯
• 中文名称: 盐酸咪奈丁
• 英文名称: amineptine hydrochloride
• 英文别名: amineptine；7-[(10,11-dihydro-5H-dibenzo[a,d]-cycloheptene-5-yl)amino]heptanoic acid hydrochloride；7-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,11,13-hexaenylamino)heptanoic acid;hydrochloride
• CAS: 30272-08-3
• 化学式: C₂₂H₂₈NO₂*Cl
• 分子量: 373.923
• InChiKey: VDPUXONTAVMIKZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.48
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  53.9
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 储存条件：
  2-8℃

反应信息

• 作为反应物：
  描述：

  硫氰酸铵 、 ammonium molybdate 、 盐酸咪奈丁 在 盐酸 、 维生素 C 作用下， 以 水 为溶剂， 生成 [amineptine(+1H)][Mo(thiocyanato)6]
  参考文献：
  名称：

  Spectrophotometric determination of trazodone, amineptine and amitriptyline hydrochlorides through ion-pair formation with molybdenum and thiocyanate

  摘要：

  Extraction spectrophotometric method has been developed for the determination of tricyclic drugs such as trazodone (TZH), amineptine (APH) and amitriptyline (ATPH) hydrochlorides in pure form and in the dosage forms coming from different Egyptian markets. The method based on the formation of ion-pairs between these drugs under investigation and inorganic complex of Mo(V)-thiocyanate followed by its extraction with methylene chloride. The optimum conditions for the ion-pairs formation are established. The method permits the determination of TZH, APH and ATPH over the concentration range of 2-28, 2-32 and 1-30 mu g ml(-1), respectively. The Sandell sensitivity (S) is found to be 0.105, 0.138 and 0.118 g cm(-2) for TZH, APH and ATPH, respectively. The SD is found to be 0.16-0.377,0.12-0.259 and 0.091-0.286 and the R.S.D. are 0.14-0.55, 0.12-0.399 and 0.095-0.485 for TZH, APH and ATPH, respectively. The method is applicable for the assay of the investigated drugs in different dosage forms and the results are in good agreement with those obtained by the official method. (c) 2006 Published by Elsevier B.V.

  DOI：

  10.1016/j.saa.2006.01.050

文献信息

• Pharmaceutical preparations based on active ingredients susceptible to illict administration
  申请人：ALTERGON S.A.

  公开号：EP1273301A2

  公开（公告）日：2003-01-08

  The present invention provides oral pharmaceutical preparations unsuitable for illicit administration to victims.

  本发明提供了不适合非法给受害者服用的口服药物制剂。
• Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression
  申请人：Sepracor Inc.

  公开号：EP2343073A2

  公开（公告）日：2011-07-13

  One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT2A modulator or DRI.

  本发明的一个方面涉及含有两种或两种以上活性剂的药物组合物，这些活性剂一起服用时可用于治疗失眠和/或抑郁症等。药物组合物的第一种成分是 GABA 受体调节化合物。药物组合物的第二种成分是血清素再摄取抑制剂、去甲肾上腺素再摄取抑制剂、5-HT2A调节剂或多巴胺再摄取抑制剂。在某些实施方案中，药物组合物包含艾佐匹克隆。在一个优选的实施方案中，药物组合物包括艾司佐匹克隆和氟西汀。本发明还涉及一种治疗睡眠异常、治疗失眠、治疗抑郁症、增强抗抑郁治疗、引起剂量节省效应、减少抑郁症复发、改善抗抑郁治疗的疗效或改善抗抑郁治疗的耐受性的方法，包括向有需要的患者联合施用GABA受体调节化合物；和SRI、NRI、5-HT2A调节剂或DRI。
• Compositions and methods for selective delivery of oligonucleotide molecules to specific neuron types
  申请人：Nlife Therapeutics S.L.

  公开号：EP2380595A1

  公开（公告）日：2011-10-26

  The invention provides a conjugate comprising (i) a nucleic acid which is complementary to a target nucleic acid sequence and which expression prevents or reduces expression of the target nucleic acid and (ii) a selectivity agent which is capable of binding with high affinity to a neurotransmitter transporter. The conjugates of the present invention are useful for the delivery of the nucleuc acid toi cell of interests and thus, for the treatment of diseases which require a down-regulation of the protein encoded by the target nucleic acid as well as for the delivery of contrast agents to the cells for diagnostic purposes.

  本发明提供了一种共轭物，该共轭物包含(i)与靶核酸序列互补的核酸，该核酸的表达可防止或减少靶核酸的表达；(ii)能够与神经递质转运体高亲和力结合的选择剂。本发明的共轭物可用于将核酸递送至相关细胞，从而治疗需要下调靶核酸编码蛋白的疾病，也可用于将造影剂递送至细胞以进行诊断。
• Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same
  申请人：Platform Brightworks Two, Ltd.

  公开号：US10028949B2

  公开（公告）日：2018-07-24

  There may be provided compositions of lipophilic pharmaceutical agents with improved solubility and stability. For example, there may be provided a non-aqueous composition that comprises a lipophilic pharmaceutical agent, and an amphiphilic polymeric solvent such as PEG400 but essentially free of organic solvents and non-solubilized particles. The composition may be further diluted with a desired aqueous diluent such as an infusion fluid for parenteral administration to a subject such as a human. The compositions may be useful for the treatment for diseases or conditions that are sensitive to lipophilic agents, such as infectious diseases, malignant or autoimmune diseases.

  可提供具有更好溶解性和稳定性的亲脂性药剂组合物。例如，可以提供一种非水性组合物，其中包括亲脂性药剂和两亲性聚合物溶剂（如 PEG400），但基本上不含有机溶剂和非增溶颗粒。该组合物可进一步用所需的水性稀释剂稀释，如输液，用于人等受试者的非肠道给药。该组合物可用于治疗对亲脂性制剂敏感的疾病或病症，如传染性疾病、恶性或自身免疫性疾病。
• Topical regional neuro-affective therapy in mammals with cannabinoids
  申请人：Afgin Pharma, LLC

  公开号：US10172809B2

  公开（公告）日：2019-01-08

  A method of treating a disease state or condition in mammals other than humans via topical brainstem afferent stimulation therapy via the administration of a cannabinoid drug(s) to the back of the neck region and/or spine to provide regional neuro-affective therapy is disclosed. In certain preferred embodiments, the cannabinoid drug(s) are not psychoactive or substantially not psychoactive. In certain embodiments, the cannabinoid drug(s) are incorporated into a pharmaceutically acceptable topical carrier, e.g., a cream or mousse. In certain preferred embodiments, the cannabinoid drug(s) comprises cannabidiol.

  本发明公开了一种通过对颈后区域和/或脊柱施用大麻素药物进行局部脑干传入刺激治疗以提供区域神经情感治疗的方法，用于治疗除人以外的哺乳动物的疾病状态或病症。在某些优选的实施方案中，大麻素药物不具有精神活性或基本不具有精神活性。在某些实施方案中，大麻素药物被掺入药学上可接受的局部载体中，例如膏霜或摩丝。在某些优选的实施方案中，大麻素药物包括大麻二酚。