N-氯-2-(1H-咪唑-5-基)乙胺 | 109241-54-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: N-氯-2-(1H-咪唑-5-基)乙胺
• 英文名称: histamine monochloramine
• 英文别名: 1H-Imidazole-4-ethanamine, N-chloro-；N-chloro-2-(1H-imidazol-5-yl)ethanamine
• CAS: 109241-54-5
• 化学式: C₅H₈ClN₃
• 分子量: 145.592
• InChiKey: YUCOVYKZDMXLIN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  40.7
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  histamine dichloride 在 sodium hypochlorite 作用下， 以 phosphate buffer 为溶剂， 反应 0.33h， 生成 N-氯-2-(1H-咪唑-5-基)乙胺
  参考文献：
  名称：

  Histamine chloramines have a persistent stimulating effect on histamine H2 receptors and gastric acid secretion

  摘要：

  Histamine plays an important role in the control of gastric acid secretion. Recently, chlorinated derivatives of histamine have been identified as having multiple effects on the intestinal tract. The aim of this study was to investigate the role of histamine chloramines on gastric acid secretion. We compared the effects of histamine and histamine chloramines on the histamine H-2 receptors in vitro using guinea pigs and on gastric acid secretion in rats. With respect to the effects on histamine H-2 receptors, histamine monochloramine showed agonist effects similar to those seen with histamine, but the agonist effects of histamine dichloramine were about half those of histamine. Unlike histamine effects, the histamine H-2 receptor agonist effects of histamine monochloramine and histamine dichloramine did not disappear after repeated washout. With respect to the stimulation of gastric acid secretion in vivo, histamine monochloramine was similar to histamine, while the effect of histamine dichloramine was 42.2-52.7% of that of histamine. The recovery time to the basal secretory level after completion of stimulation by histamine chloramines was significantly prolonged compared with histamine. These results suggest that histamine chloramines, which bind strongly with histamine H-2 receptors, may delay the termination of gastric acid secretion and increase the burden on the gastric and duodenal mucosa.

  DOI：

  10.1016/0014-2999(94)00773-z

文献信息

• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT OF PAIN<br/>[FR] MÉTHODES ET COMPOSITIONS POUR LE TRAITEMENT DE LA DOULEUR
  申请人：HELLER ADAM

  公开号：WO2010017405A1

  公开（公告）日：2010-02-11

  The invention features methods, kits, and compositions for the treatment of pain.

  本发明涉及用于治疗疼痛的方法、试剂盒和组合物。
• Farnesyl protein transferase inhibitors
  申请人：Kelly M. Joseph

  公开号：US20070213340A1

  公开（公告）日：2007-09-13

  Disclosed are compounds of the formula: wherein R 13 represents an imidazole ring; R 14 represents a carbamate, urea, amide or sulfonamide group, and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.