氯普唑仑甲磺酸盐 | 61197-93-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 中文名称: 氯普唑仑甲磺酸盐
• 英文名称: 1H-Imidazo(1,2-a)(1,4)benzodiazepin-1-one, 6-(2-chlorophenyl)-2,4-dihydro-2-((4-methyl-1-piperazinyl)methylene)-8-nitro-, methanesulphonate
• 英文别名: (2E)-6-(2-chlorophenyl)-2-[(4-methylpiperazin-1-yl)methylidene]-8-nitro-4H-imidazo[1,2-a][1,4]benzodiazepin-1-one;methanesulfonic acid
• CAS: 61197-93-1
• 化学式: C24H25ClN6O6S
• 分子量: 561.0
• InChiKey: DDSDPQHQLNAGLJ-UGAWPWHASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.44
• 重原子数：
  38
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  160
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• COMBINATION PRODUCT FOR THE INDUCTION AND/OR MAINTENANCE OF GENERAL ANESTHESIA
  申请人：BlumenTech S.L.

  公开号：EP3773723A1

  公开（公告）日：2021-02-17
• US7927613B2
  申请人：——

  公开号：US7927613B2

  公开（公告）日：2011-04-19
• [EN] COMBINATION PRODUCT FOR THE INDUCTION AND/OR MAINTENANCE OF GENERAL ANESTHESIA<br/>[FR] PRODUIT DE COMBINAISON POUR L'INDUCTION ET/OU LA MAINTENANCE D'UNE ANESTHÉSIE GÉNÉRALE
  申请人：BLUMENTECH S L

  公开号：WO2019197594A1

  公开（公告）日：2019-10-17

  The state of general anesthesia (GA) is essential to many surgical and medical procedures. This state is characterized by loss of consciousness, deep analgesia and suppression of movements. GA is rarely achieved with a single drug, usually requiring the combination of various pharmacological agents. Each drug can interact with one or more molecular targets affecting neuronal excitability and synaptic transmission in multiple regions of the CNS. Agonists of the μ-opioid receptor are commonly used in GA to cause analgesia, but not to induce or maintain loss of consciousness or movement suppression. Additionally, agonists of the μ-opioid receptor can cause serious unwanted side effects, e.g. respiratory depression. The present invention provides alternative combination products based on K- opioid receptor agonists. These combination products unexpectedly induced loss of consciousness, and were able to achieve and maintain GA. Furthermore, the combination products supressed pain perception without the need of a μ-opioid receptor agonist. The combination of Salvinorin A, a selective κ-opioid receptor agonist, with Diazepam or Medetomidine surprisingly led to rapid consciousness, deep analgesia and movement suppression. This combination was found to effectively induce and maintain a state of general anesthesia.