2-Methyl-5-(1H-tetrazol-5-yl)-pyrazine | 343787-71-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-Methyl-5-(1H-tetrazol-5-yl)-pyrazine
• 英文别名: 2-methyl-5-(2H-tetrazol-5-yl)pyrazine
• CAS: 343787-71-3
• 化学式: C₆H₆N₆
• 分子量: 162.154
• InChiKey: CKRDSNDHOKHGBP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.6
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  80.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-Methyl-5-(1H-tetrazol-5-yl)-pyrazine 在 双氧水 、 溶剂黄146 作用下， 反应 6.0h， 生成 2-Methyl-5-(1H-tetrazol-5-yl)-pyrazine 1-oxide
  参考文献：
  名称：

  Ambrogi; Cozzi; Sanjust, European Journal of Medicinal Chemistry, 1980, vol. 15, # 2, p. 157 - 163

  摘要：

  DOI：

文献信息

• Compositions For Treating Flushing And Lipid-Associated Disorders Comprising Niacin Receptor Partial Agonists
  申请人：Behan Dominic P.

  公开号：US20080139628A1

  公开（公告）日：2008-06-12

  The invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist. In addition, the invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and an effective lipid altering amount of niacin or a niacin analog. The invention further provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist and subsequently administering to said subject an effective lipid altering amount of niacin or a niacin analog.

  本发明提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂。此外，本发明还提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂和有效改变脂质含量的烟酸或烟酸类似物。本发明进一步提供了一种减少烟酸或烟酸类似物引起的面红的方法，包括向该受体中注射有效减少面红量的烟酸受体部分激动剂，然后向该受体中注射有效改变脂质含量的烟酸或烟酸类似物。
• Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders
  申请人：Arena Pharmaceuticals, Inc.

  公开号：US20040142377A1

  公开（公告）日：2004-07-22

  The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

  本发明涉及鉴定候选化合物是否为 G 蛋白偶联受体（GPCR）调节剂的方法。在优选的实施方案中，GPCR 是人类的。在其他优选的实施方案中，GPCR 与 Gi 相耦合，降低细胞内 cAMP 的水平。在其他优选的实施方案中，GPCR 由脂肪细胞内源表达。在更多优选的实施方案中，GPCR 可抑制细胞内脂肪分解。在其他更优选的实施方案中，GPCR 是烟酸受体。本发明还涉及使用所述 GPCR 的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病的治疗剂，包括血脂异常、动脉粥样硬化、冠心病、中风、胰岛素抵抗和 2 型糖尿病。
• AMBROGI V.; COZZI P.; SANIUST P.; BERTONE L.; LOVISOLO P. P.; BRIATICO G.+, EUR. J. MED. CHEM.-CHIM. THER., 1980, 15, NO 2, 157-163
  作者：AMBROGI V.、 COZZI P.、 SANIUST P.、 BERTONE L.、 LOVISOLO P. P.、 BRIATICO G.+

  DOI：——

  日期：——
• COMPOSITIONS FOR TREATING FLUSHING AND LIPID-ASSOCIATED DISORDERS COMPRISING NIACIN RECEPTOR PARTIAL AGONISTS
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1811996A1

  公开（公告）日：2007-08-01
• Human G Protein-Coupled Receptors and Modulators Thereof for the Treatment of Metabolic-Related Disorders
  申请人：Unett David J.

  公开号：US20110177612A1

  公开（公告）日：2011-07-21

  The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.