SKF 38393 | 1000004-68-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: SKF 38393
• 英文别名: (+/-)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride；SKF 38393 hydrochloride；2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine hydrochloride；1-phenyl-7,8-dihydroxy-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride；(±)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrochloride；(±)-SKF-38393 hydrochloride；hydron;5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;chloride
• CAS: 1000004-68-1
• 化学式: C₁₆H₁₇NO₂*ClH
• 分子量: 291.777
• InChiKey: YEWHJCLOUYPAOH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  52.5
• 氢给体数：
  4
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  SKF 38393 在 sodium hypochlorite 、 sodium hydrogensulfite 作用下， 以 盐酸 为溶剂， 生成 6,9-Dichloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride
  参考文献：
  名称：

  Benz-tetrasubstituted 1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines

  摘要：

  一组6,9-二取代-7,8-二羟基-1-苯基-2,3,4,5-四氢-1H-3-苯并哌啶具有多巴胺活性。该发明的主要物种示例是6,9-二氯-7,8-二羟基-1-苯基-2,3,4,5-四氢-1H-3-苯并哌啶和6,9-二氯-7,8-二羟基-1-(对羟基苯基)-2,3,4,5-四氢-1H-3-苯并哌啶的酸盐形式。

  公开号：

  US04171359A1
• 作为产物：
  描述：

  (±)-1-苯基-2,3,4,5-四氢-(1H)-3-苯并ze庚因-7,8-二醇氢溴酸盐 、 盐酸 生成 SKF 38393
  参考文献：
  名称：

  KAISER, C.;DANDRIDGE, P. A.;GARVEY, E.;HAHN, R. A.;SARAU, H. M.;SETLER, P+, J. MED. CHEM., 1982, 25, N 6, 697-703

  摘要：

  DOI：

文献信息

• Dopamine analog amide
  申请人：——

  公开号：US20010056116A1

  公开（公告）日：2001-12-27

  The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

  该发明涉及使用脂肪酸载体和神经活性药物形成前药。该前药在胃和血液流动环境中稳定，并可通过口服递送。该前药容易穿过血脑屏障。一旦进入中枢神经系统，前药被水解成脂肪酸载体和药物以释放药物。在首选实施方式中，载体是4,7,10,13,16,19二十二碳六烯酸，药物是多巴胺。两者都是中枢神经系统的正常成分。药物和载体之间的共价键通常是酰胺键，这种键可以在胃的条件下存活。因此，前药可以被摄入，并且不会在胃中完全水解成载体分子和药物分子。
• METHODS OF TREATING VASCULAR DISEASES USING BROMOCRIPTINE
  申请人：VeroScience LLC

  公开号：EP3090745A1

  公开（公告）日：2016-11-09

  The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, a pro-coagulative state, and insulin resistance (with or without treating obesity or endothelial dysfunction), associated with or independent from Metabolic Syndrome, as well as vascular disease such as cardiovascular, cerebrovascular, or peripheral vascular disease comprising the step of administering to a patient suffering from such disorders a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

  本发明涉及一种同时治疗高血压、高甘油三酯血症、促炎症状态、促凝血状态和胰岛素抵抗（治疗或不治疗肥胖或内皮功能障碍）（与代谢综合征有关或无关）以及心血管、脑血管或外周血管疾病等血管疾病的方法，该方法包括向患有此类疾病的患者施用治疗有效量的中枢作用多巴胺激动剂。在一个实施方案中，中枢作用多巴胺激动剂是溴隐亭，可选择与药学上可接受的载体结合使用。
• Therapeutic treatment for the metabolic syndrome and type 2 diabetes
  申请人：——

  公开号：US20040077679A1

  公开（公告）日：2004-04-22

  The present invention is directed to a method for treating the metabolic syndrome or Type 2 diabetes, comprising the step of administering to a subject in need of such treatment a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject. The present invention is also directed to a method for treating the metabolic syndrome or Type 2 diabetes, comprising the step of administering to a subject in need of such treatment at least one compound that simultaneously stimulates (1) an increase in central dopaminergic neuronal activity level, and (2) a decrease in central noradrenergic neuronal activity level. The present invention is also directed to pharmaceutical compositions that include the above compounds and a pharmaceutically acceptable carrier.

  本发明涉及一种治疗代谢综合征或2型糖尿病的方法，包括向需要这种治疗的受试者施用药物组合物的步骤，该药物组合物包含(1)至少一种刺激受试者中枢多巴胺能神经元活性水平增加的化合物，和(2)至少一种刺激受试者中枢去甲肾上腺素能神经元活性水平降低的化合物。本发明还涉及一种治疗代谢综合征或 2 型糖尿病的方法，该方法包括以下步骤：向需要治疗的受试者施用至少一种化合物，该化合物可同时刺激(1)中枢多巴胺能神经元活性水平的升高和(2)中枢去甲肾上腺素能神经元活性水平的降低。本发明还涉及包括上述化合物和药学上可接受的载体的药物组合物。
• Methods of treating metabolic syndrome using dopamine receptor agonists
  申请人：——

  公开号：US20040220190A1

  公开（公告）日：2004-11-04

  The present invention is directed to a method of simultaneously treating hypertension, hypertriglyceridemia, a pro-inflammatory state, and insulin resistance (with or without treating obesity), associated with Metabolic Syndrome, comprising the step of administering to a patient suffering from Metabolic Syndrome a therapeutically effective amount of a central acting dopamine agonist. In one embodiment, the central acting dopamine agonist is bromocriptine, optionally combined with a pharmaceutically acceptable carrier.

  本发明涉及一种同时治疗与代谢综合征有关的高血压、高甘油三酯血症、促炎症状态和胰岛素抵抗（治疗或不治疗肥胖）的方法，包括向代谢综合征患者施用治疗有效量的中枢作用多巴胺激动剂。在一个实施方案中，中枢作用多巴胺激动剂是溴隐亭，可选择与药学上可接受的载体结合使用。
• Therapeutic treatment for the metabolic syndrome, type2 diabetes, obesity, or prediabetes
  申请人：Cincotta H. Anthony

  公开号：US20050054734A1

  公开（公告）日：2005-03-10

  The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic neuronal activity within the hypothalamus of the central nervous system of the patient. In another aspect, the present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of: administering to a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes a pharmaceutical composition comprising (1) at least one compound that stimulates an increase in central dopaminergic neuronal activity level in the subject, and (2) at least one compound that stimulates a decrease in central noradrenergic neuronal activity level in the subject. The present invention is also directed to pharmaceutical compositions that include the above compounds and a pharmaceutically acceptable carrier.

  本发明涉及一种治疗代谢综合征、2型糖尿病、肥胖或糖尿病前期患者的方法，包括增加患者中枢神经系统下丘脑内多巴胺能神经元与去甲肾上腺素能神经元活性的比率。在另一方面，本发明涉及一种治疗患有代谢综合征、2 型糖尿病、肥胖症或糖尿病前期的患者的方法，包括以下步骤：给患有代谢综合征、2 型糖尿病、肥胖症或糖尿病前期的患者施用药物组合物，该药物组合物包含(1)至少一种刺激受试者中枢多巴胺能神经元活性水平增加的化合物，和(2)至少一种刺激受试者中枢去甲肾上腺素能神经元活性水平降低的化合物。本发明还涉及包括上述化合物和药学上可接受的载体的药物组合物。