4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-1,3-dihydroisoindol-2-amine;hydron;chloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-1,3-dihydroisoindol-2-amine;hydron;chloride
• 化学式: C11H14Cl2N4
• 分子量: 273.16
• InChiKey: RBRKIFULRBQIGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.54
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  39.7
• 氢给体数：
  3
• 氢受体数：
  2

文献信息

• Use of alpha 2 adrenergic receptor antagonists for the production of pharmaceutical compositions for treating colonic spasm, irritable bowel syndrome and constipation and process for preparing such pharmaceutical compositions
  申请人：Merck & Co., Inc.

  公开号：EP0216247A2

  公开（公告）日：1987-04-01

  Selective α₂-adrenergic receptor antagonists are effective in modifying gastro-­intestinal motility in a manner useful in the treatment of colonic spasm, irritable bowel syndrome and constipation.

  选择性α₂-肾上腺素能受体拮抗剂能有效改变胃肠道的蠕动，从而治疗结肠痉挛、肠易激综合征和便秘。
• Use of edg-receptor agonists for the treatment of hypertension
  申请人：Molderings J Gerhard

  公开号：US20050232860A1

  公开（公告）日：2005-10-20

  Treatment and/or prophylaxis of hypertension involving administering a therapeutically active amount of an edg-receptor agonist or a pharmaceutically acceptable salt thereof. Preferably the edg-receptor agonist is a highly selective I 1 -receptor agonist and essentially devoid of α 2 -receptor agonist activity and has an imidazoline structure. Hence, hypertension may be treated without causing α 2 -receptor induced side effects. The invention also provides appropriate screening tools for identifying compounds acting with high selectivity as I 1 -receptor agonists however lacking α 2 -receptor induced side effects. Furthermore, the receptor, membranes and cells comprising said receptor, and assays for screening compounds with said receptor are discussed in the context of the invention.

  治疗和/或预防高血压，包括施用治疗活性量的edg-受体激动剂或其药学上可接受的盐。最好是高选择性的 I 1 -受体激动剂，并且基本上不含 α 2 -受体激动剂活性，并具有咪唑啉结构。因此，在治疗高血压时不会引起α 2 -受体激动剂的活性。 2 -受体引起的副作用。本发明还提供了适当的筛选工具，用于鉴定具有高选择性 I 1 -受体激动剂但缺乏 α 2 -受体诱导的副作用。此外，本发明还讨论了受体、包含所述受体的膜和细胞，以及用所述受体筛选化合物的检测方法。
• EDG-RECEPTOR AGONISTS FOR THE TREATMENT OF HYPERTENSION
  申请人：Solvay Pharmaceuticals GmbH

  公开号：EP1490111A2

  公开（公告）日：2004-12-29
• US4673680A
  申请人：——

  公开号：US4673680A

  公开（公告）日：1987-06-16
• [EN] USE OF EDG-RECEPTOR AGONISTS FOR THE TREATMENT OF HYPERTENSION<br/>[FR] UTILISATION D'AGONISTES DE RECEPTEUR EDG POUR LE TRAITEMENT DE L'HYPERTENSION
  申请人：SOLVAY PHARM GMBH

  公开号：WO2003051395A2

  公开（公告）日：2003-06-26

  Treatment and /or prophylaxis of hypertension involving administering a therapeutically active amount of an edg-receptor agonist or a pharmaceutically acceptable salt thereof. Preferably the edg-receptor agonist is a highly selective l1-receptor agonist and essentially devoid of α2-receptor agonist activity and has an imidazoline structure. Hence, hypertension may be treated without causing α2-receptor induced side effects. The invention also provides appropriate screening tools for identifying compounds acting with high selectivity as l1-receptor agonists however lacking α2-receptor induced side effects. Furthermore, the receptor, membranes and cells comprising said receptor, and assays for screening compounds with said receptor are discussed in the context of the invention.