6-氯-2,3-二氢-5-甲基-N-[6-[((2-甲基-3-吡啶基)氧基]-3-吡啶基]-1H-吲哚-1-羧酰胺二盐酸盐 | 1049747-87-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 6-氯-2,3-二氢-5-甲基-N-[6-[((2-甲基-3-吡啶基)氧基]-3-吡啶基]-1H-吲哚-1-羧酰胺二盐酸盐
• 中文别名: 6-氯-2,3-二氢-5-甲基-N-[6-[(2-甲基-3-吡啶基)氧]-3-吡啶基]-1H-吲哚-1-酰胺盐酸盐
• 英文名称: 6-Chloro-5-methyl-N-(6-((2-methylpyridin-3-yl)oxy)pyridin-3-yl)indoline-1-carboxamide dihydrochloride
• 英文别名: 6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide;dihydrochloride
• CAS: 1049747-87-6
• 化学式: C21H21Cl3N4O2
• 分子量: 467.8
• InChiKey: GCMNSEILNIPNSX-UHFFFAOYSA-N

物化性质

• 溶解度：
  乙醇:1.0(最大浓度 mg/mL);2.14(最大浓度 mM)PBS (pH 7.2):10.0(最大浓度 mg/mL);21.38(最大浓度 mM) DMSO:59.63(最大浓度 mg/mL);127.47(最大浓度 mM)DMF:30.0(最大浓度 mg/mL);64.13(最大浓度 mM)

计算性质

• 辛醇/水分配系数(LogP)：
  5.98
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  67.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335

制备方法与用途

生物活性：SB 242084盐酸盐是5-HT2C选择性抑制剂，其pKi值为9.0，对5-HT2A和5-HT2B受体的作用弱100倍以上。

靶点：

受体	5-HT₂₃受体
pKi 值	9.0

文献信息

• Use of dopamine and serotonin receptor antagonists for treatment in a subject with retinal degeneration
  申请人：United States Government as Represented by The Department of Veterans Affairs

  公开号：US11033554B2

  公开（公告）日：2021-06-15

  Disclosed herein are methods of treating disorders of the retina (e.g., macular degeneration, retinitis pigmentosa, etc.) comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound (for example, an antipsychotic drug) that blocks or diminishes agonist-mediated responses upon binding to either dopamine D2-like receptors or serotonin 5-HT2 receptors.

  本文公开了治疗视网膜疾病（如黄斑变性、视网膜色素变性等）的方法，包括向需要此类治疗的受试者施用治疗有效量的化合物（例如抗精神病药物），该化合物可阻断或减少与多巴胺D2样受体或5-羟色胺5-HT2受体结合后激动剂介导的反应。
• USE OF DOPAMINE AND SEROTONIN RECEPTOR ANTAGONISTS FOR TREATMENT IN A SUBJECT WITH RETINAL DEGENERATION
  申请人：United States Government as Represented by The Department of Veterans Affairs

  公开号：US20170020891A1

  公开（公告）日：2017-01-26

  Disclosed herein are methods of treating disorders of the retina (e.g., macular degeneration, retinitis pigmentosa, etc.) comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound (for example, an antipsychotic drug) that blocks or diminishes agonist-mediated responses upon binding to either dopamine D2-like receptors or serotonin 5-HT2 receptors.