盐酸埃他卡林 | 642407-63-4

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 盐酸埃他卡林
• 英文名称: Iptakalim hydrochloride
• 英文别名: N-(1-methylethyl)-1,1,2-trimethyl-propylamine hydrochloride；N-(1-methylethyl)-2,3-dimethyl-2-butylamine hydrochloride；2,3-dimethyl-N-propan-2-ylbutan-2-amine;hydrochloride
• CAS: 642407-63-4
• 化学式: C₉H₂₁N*ClH
• 分子量: 179.733
• InChiKey: RXNJQAYLNOXYKW-UHFFFAOYSA-N

物化性质

• 溶解度：
  水：25 mg/mL（139.10 mM；超声加热并加热至 70°C）

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  16.6
• 氢给体数：
  1
• 氢受体数：
  1

制备方法与用途

盐酸依他卡林是一种亲脂性的对氨基化合物，它是一种新型的ATP敏感性钾通道（KATP）开放剂，同时也是一种含α4β2亚单位的烟碱乙酰胆碱受体（nAChR）拮抗剂。

反应信息

• 作为反应物：
  描述：

  盐酸埃他卡林 、 2-(2,4,5-trichlorophenoxy)acetyl chloride 在 4-二甲氨基吡啶 三乙胺 作用下， 以 甲苯 为溶剂， 反应 14.0h， 以86.8%的产率得到N-(1-methylethyl)-N-(2,4,5-trichlorophenoxy-acetyl)-2,3-dimethyl-2-butylamine
  参考文献：
  名称：

  AMINE DERIVATIVE WITH POTASSIUM CHANNEL REGULATORY FUNCTION, ITS PREPARATION AND USE

  摘要：

  公开号：

  EP1386908B1
• 作为产物：
  描述：

  Iptakalim 在 盐酸 作用下， 以 乙醇 、 水 为溶剂， 以95.5%的产率得到盐酸埃他卡林
  参考文献：
  名称：

  AMINE DERIVATIVE WITH POTASSIUM CHANNEL REGULATORY FUNCTION, ITS PREPARATION AND USE

  摘要：

  公开号：

  EP1386908B1

文献信息

• Amine derivative with potassium channel regulatory function, its preparation and use
  申请人：——

  公开号：US20040266822A1

  公开（公告）日：2004-12-30

  The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression. 1

  本发明提供了由式I表示的胺衍生物，其异构体、拉克酸盐或光学异构体，其酰胺或酯，以及含有该化合物的制药组合物及其制备方法。本发明还涉及上述化合物在预防或治疗心血管疾病、糖尿病、支气管和尿道平滑肌痉挛以及缺血性和缺氧性神经损伤的药物制剂中的应用。上述化合物可用于治疗高血压、心绞痛、心肌梗死、充血性心力衰竭、心律失常、糖尿病、痉挛性支气管疾病、痉挛性膀胱或输尿管疾病以及抑郁症。
• Intranasal administration of modulators of hypothalamic ATP-sensitive potassium channels
  申请人：Herlands Louis

  公开号：US20070026079A1

  公开（公告）日：2007-02-01

  Provided are methods of increasing K ATP channel activity in the hypothalamus of a mammal, methods of reducing glucose production in a mammal, methods of reducing peripheral glucose levels in a mammal, methods of reducing triglyceride levels in a mammal, methods of reducing very low density lipoprotein (VLDL) levels in a mammal, methods of methods of reducing gluconeogenesis in the liver of a mammal, methods of treating metabolic disorders such as diabetes, hyperglycemia, insulin resistance, glucose intolerance, metabolic syndrome and/or obesity, and methods of increasing glucose production and peripheral glucose levels in a mammal. Also provided are methods of treating heart failure, ischemia, coronary heart disease, familial lipoprotein lipase deficiency, hypopituitarism, hyperlipidemia, hypertriglyceridemia, hyperVLDLemia, atherosclerosis, hypercholesterolemia, hypertension, polycystic ovary syndrome, gonadotropin deficiency and/or amenorrhea.
• Method for Decreasing Blood Glucose Levels
  申请人：Wu Jie

  公开号：US20070231273A1

  公开（公告）日：2007-10-04

  A method for decreasing blood glucose levels is disclosed. Iptakalim hydrochloride (a SUR1 subunit-dependent K ATP channel blocker and a SUR2 subunit-selective K ATP channel opener) is used to block pancreatic β-cell K ATP channels, which depolarizes β-cells, elevates intracellular Ca 2+ concentrations, and in turn increases insulin release. Therefore, in some implementations, iptakalim hydrochloride is an optimal treatment for type-2 diabetic patients with cardiovascular disorders.
• Modulation of Hypothalamic Atp-Sensitive Potassium Channels
  申请人：Rossetti Luciano

  公开号：US20090012067A1

  公开（公告）日：2009-01-08

  Provided are methods of increasing K ATP activity in the hypothalamus of a mammal, methods of reducing glucose production and peripheral blood glucose levels in a mammal, methods of inhibiting gluconeogenesis in the liver of a mammal, and methods of increasing glucose production and peripheral blood glucose levels in a mammal.
• US7560473B2
  申请人：——

  公开号：US7560473B2

  公开（公告）日：2009-07-14