1-Demethylmethergoline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-Demethylmethergoline
• 英文别名: 6-methyl-8β-carbobenzyloxy-aminomethyl-10α-ergoline；(7-Methyl-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-ylmethyl)-carbamic acid benzyl ester；benzyl N-[[(6aR,9S,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methyl]carbamate
• 化学式: C₂₄H₂₇N₃O₂
• 分子量: 389.497
• InChiKey: REJFPXMKRRYBSC-UCNVEGJOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  57.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  6-甲基麦角灵-8β-甲醇 在 TEA 、 三苯基膦 、 肼 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 2.0h， 生成 1-Demethylmethergoline
  参考文献：
  名称：

  Serotonergic ergoline derivatives

  摘要：

  Novel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT1A or 5-HT2 affinity and selectivity respectively. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00166-8

文献信息

• Dopamine agonists for treating type II diabetes
  申请人：LOUISIANA STATE UNIVERSITY AGRICULTURAL AND MECHANICAL COLLEGE

  公开号：EP0440333A2

  公开（公告）日：1991-08-07

  A process for the long term modification and regulation of lipid metabolism -- generally to reduce obesity, insulin resistance, and hyperinsulinemia or hyperglycemia, or both (these are the hallmarks of noninsulin dependent, or Type II diabetes) -- by administratlon (i.e., by feed or injection into the bloodstream) to a vertebrate, animal or human, of a dopamine agonist, e.g., bromocriptine. Administration of the bromocriptine is made over a limited period at a time of day dependent on the normal circadian rhythm of fat and lean members of a similar species. Decreases in body fat deposits result by treatment of an obese species on a daily timed sequence based on circadian rhythms of the peak prolactin, or peak prolactin and peak glucocorticosteroid, blood level established for lean members of a similar species. Insulin resistance, and hyperinsulinemia and hyperglycemia, or both, can also be controlled in humans on a long term basis by treatment corresponding to that of the treatment for obesity. The short term daily injections reset hormonal timing in the neural centers of the brain to produce long term effects.

  一种长期改变和调节脂质代谢的方法--通常用于减少肥胖、胰岛素抵抗和高胰岛素血症或高血糖，或两者兼而有之（这些都是非胰岛素依赖型糖尿病或 II 型糖尿病的特征）--方法是通过给脊椎动物（动物或人）注射多巴胺激动剂，如溴隐亭（bromocriptine）（即通过喂食或注射到血液中）。溴隐亭的给药时间是有限制的，每天的给药时间取决于类似物种中肥瘦成员的正常昼夜节律。根据泌乳素峰值或泌乳素峰值和糖皮质激素峰值的昼夜节律，对肥胖物种进行每日定时治疗，可减少体内脂肪沉积。胰岛素抵抗、高胰岛素血症和高血糖或两者都有，也可以通过与肥胖症治疗方法相对应的治疗方法长期控制。每日短期注射可重置大脑神经中枢的荷尔蒙时间，从而产生长期效果。
• Use of dipeptidylpetidase inhibitors to regulate glucose metabolism
  申请人：TRUSTEES OF TUFTS COLLEGE

  公开号：EP1520582A2

  公开（公告）日：2005-04-06

  The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis.

  本发明提供了用于改变和调节葡萄糖和脂质代谢的方法和组合物，一般用于减少胰岛素抵抗、高血糖、高胰岛素血症、肥胖、高脂血症、高脂蛋白血症（如乳糜微粒、VLDL 和 LDL），以及调节体内脂肪和更一般的脂质储存，更一般地说，用于改善代谢紊乱，特别是与糖尿病、肥胖和/或动脉粥样硬化有关的代谢紊乱。
• Use of dipeptidylpeptidase inhibitors to regulate glucose metabolism
  申请人：Trustees Of Tufts College

  公开号：EP2433623A1

  公开（公告）日：2012-03-28

  The present invention provides inhibitor of dipeptidylpeptidase IV (DPIV) for use for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis.

  本发明提供了二肽基肽酶 IV（DPIV）抑制剂，用于改变和调节葡萄糖和脂质代谢，一般用于减少胰岛素抵抗、高血糖、高胰岛素血症、肥胖、高脂血症、高脂蛋白血症（如乳糜微粒、VLDL 和 LDL），以及调节体内脂肪和更普遍的脂质储存，更普遍的是改善代谢紊乱，尤其是与糖尿病、肥胖和/或动脉粥样硬化相关的紊乱。
• Use of prolactin-inhibiting compounds for resetting the prolactin circadian rhythm
  申请人：LOUISIANA STATE UNIVERSITY AGRICULTURAL AND MECHANICAL COLLEGE

  公开号：EP0440333B1

  公开（公告）日：1998-12-23
• Process for the long term reduction of body fat stores, insulin resistance, hyperinsulinemia and hypoglycemia in vertebrates
  申请人：LOUISIANA STATE UNIVERSITY AGRICULTURAL AND MECHANICAL COLLEGE

  公开号：EP0917874B1

  公开（公告）日：2008-04-09