8,16-bis-(4-nitro-phenyl)-5,6,8,8a,13,14,16,16a-octahydro-[1,2,4,5]tetrazino[6,1-a;3,4-a']diisoquinoline | 33454-27-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: 8,16-bis-(4-nitro-phenyl)-5,6,8,8a,13,14,16,16a-octahydro-[1,2,4,5]tetrazino[6,1-a;3,4-a']diisoquinoline
• 英文别名: 2,13-Bis(4-nitrophenyl)-1,2,12,13-tetrazapentacyclo[12.8.0.03,12.04,9.015,20]docosa-4,6,8,15,17,19-hexaene；2,13-bis(4-nitrophenyl)-1,2,12,13-tetrazapentacyclo[12.8.0.03,12.04,9.015,20]docosa-4,6,8,15,17,19-hexaene
• CAS: 33454-27-2
• 化学式: C₃₀H₂₆N₆O₄
• 分子量: 534.574
• InChiKey: INANJKXOVAVHEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.1
• 重原子数：
  40
• 可旋转键数：
  2
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  105
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  三氯乙醛 、 8,16-bis-(4-nitro-phenyl)-5,6,8,8a,13,14,16,16a-octahydro-[1,2,4,5]tetrazino[6,1-a;3,4-a']diisoquinoline 生成 3-(4-nitro-phenyl)-2-trichloromethyl-2,3,6,10b-tetrahydro-5H-[1,3,4]oxadiazolo[2,3-a]isoquinoline
  参考文献：
  名称：

  Grashey,R.; Adelsberger,K., Angewandte Chemie, 1962, vol. 74, # 8, p. 292 - 293

  摘要：

  DOI：

文献信息

• Treatments for female sexual dysfunction and methods for identifying compounds useful for treating female sexual dysfunction
  申请人：——

  公开号：US20030083228A1

  公开（公告）日：2003-05-01

  The present invention provides a method of treating female sexual dysfunction, the method comprising the step of administering to a patent, having or at risk of having one or more of the disorders or conditions associated with female sexual dysfunction, a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of female sexual dysfunction, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.

  本发明提供了一种治疗女性性功能障碍的方法，该方法包括向患有或有可能患有与女性性功能障碍相关的一种或多种疾病或病况的患者施用一种治疗有效量的化合物，该化合物减弱了agouti相关蛋白与黑素皮质素受体的结合，但不影响α-黑素细胞刺激激素与黑素皮质素受体的结合。本发明还提供了一种识别对治疗或预防女性性功能障碍有用的化合物的方法，该方法包括以下步骤：1）确定化合物是否影响agouti相关蛋白与黑素皮质素受体的结合；2）确定化合物是否影响α-黑素细胞刺激激素与黑素皮质素受体的结合；以及3）选择一种减弱agouti相关蛋白与黑素皮质素受体结合的化合物，但不影响α-黑素细胞刺激激素与黑素皮质素受体的结合。
• Uses of agrp-melanocortin receptor binding modulating compounds
  申请人：Pfizer Products Inc.

  公开号：EP1125579A2

  公开（公告）日：2001-08-22

  The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of α-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of α-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of α-melanocyte stimulating hormone to melanocortin receptors.

  本发明提供了一种治疗肥胖、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合征、肾上腺功能障碍、高血压、高胆固醇血症、动脉粥样硬化、高脂蛋白血症、高甘油三酯血症或药物滥用的方法、该方法包括以下步骤：向患有或有可能患有上述疾病之一的专利人施用治疗有效量的化合物，该化合物能减弱激动相关蛋白与黑皮素受体的结合，但不能减弱α-黑素细胞刺激素与黑皮素受体的结合。本发明还提供了一种鉴定化合物的方法，该化合物可用于治疗或预防肥胖、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合征、肾上腺功能障碍、高血压、高胆固醇血症、动脉粥样硬化、高脂蛋白血症、高甘油三酯血症或药物滥用，该方法包括以下步骤：1）确定一种化合物是否会影响激动相关蛋白与黑色素皮质受体的结合；2）确定一种化合物是否会影响α-促黑色素细胞激素与黑色素皮质受体的结合；以及3）选择一种能减弱激动相关蛋白与黑色素皮质受体的结合，但不影响α-促黑色素细胞激素与黑色素皮质受体的结合的化合物。
• Treatments for female sexual dysfunction
  申请人：Pfizer Productors Inc.

  公开号：EP1285658A2

  公开（公告）日：2003-02-26

  The present invention provides a method of treating female sexual dysfunction, the method comprising the step of administering to a patent, having or at risk of having one or more of the disorders or conditions associated with female sexual dysfunction, a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of α-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of female sexual dysfunction, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of α-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of α-melanocyte stimulating hormone to melanocortin receptors.

  本发明提供了一种治疗女性性功能障碍的方法，该方法包括以下步骤：向患有或有可能患有一种或多种与女性性功能障碍相关的疾病或病症的专利人施用治疗有效量的化合物，该化合物可减弱激动相关蛋白与黑色素皮质受体的结合，但不会减弱α-黑色素细胞刺激素与黑色素皮质受体的结合。本发明还提供了一种鉴定有助于治疗或预防女性性功能障碍的化合物的方法，该方法包括以下步骤：1）确定一种化合物是否影响激动相关蛋白与黑皮素受体的结合；2）确定一种化合物是否影响α-促黑皮细胞激素与黑皮素受体的结合；以及3）选择一种能减弱激动相关蛋白与黑皮素受体的结合，但不影响α-促黑皮细胞激素与黑皮素受体的结合的化合物。
• US6451783B1
  申请人：——

  公开号：US6451783B1

  公开（公告）日：2002-09-17
• US6734175B2
  申请人：——

  公开号：US6734175B2

  公开（公告）日：2004-05-11