Dinoxyline | 757176-96-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: Dinoxyline
• 英文别名: 8-oxa-15-azatetracyclo[7.7.1.02,7.013,17]heptadeca-2(7),3,5,9,11,13(17)-hexaene-5,6-diol
• CAS: 757176-96-8
• 化学式: C₁₅H₁₃NO₃
• 分子量: 255.27
• InChiKey: QOHSTVKJXZTEOL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  61.7
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• CHROMENO[4,3,2-DE]ISOQUINOLINES AS POTENT DOPAMINE RECEPTOR LIGANDS
  申请人：Nichols E. David

  公开号：US20050080266A1

  公开（公告）日：2005-04-14

  Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

  本发明涉及一种新型的多巴胺受体配体，其化学式为：该类化合物的药物配方以及使用该类化合物治疗中枢或外周神经系统多巴胺相关功能障碍的患者的方法也被描述。该类化合物预计可用于治疗帕金森病、改善认知能力、改善记忆、改善精神分裂症的负性症状、改善注意力缺陷过动症和相关的发育障碍、治疗物质滥用障碍，以及治疗各种外围病症，其中多巴胺受体占据的变化会影响生理功能，包括器官灌注、心血管功能以及选择性的内分泌和免疫系统功能。
• Method of treatment of dopamine-related dysfunction
  申请人：Mailman B. Richard

  公开号：US20050232870A1

  公开（公告）日：2005-10-20

  The present invention relates to the treatment of dopamine-related dysfunction using full D 1 dopamine receptor agonists in an intermittent dosing protocol with a short, but essential, “off-period.” The D 1 agonist concentration is reduced during the “off-period” to obtain a plasma concentration of agonist that suboptimally activates D 1 dopamine receptors for a period of time to prevent induction of tolerance. Specifically, the method comprises the steps of periodically administering to a patient a full D 1 agonist with a half-life of up to about 6 hours at a dose resulting in a first plasma concentration of agonist capable of activating D 1 dopamine receptors to produce a therapeutic effect. The dose is reduced at least once every 24 hours to obtain a second lower plasma concentration of agonist that results in suboptimal activation of D 1 dopamine receptors for a period of time sufficient to prevent induction of tolerance.

  本发明涉及使用全D1多巴胺受体激动剂在间歇性给药方案中治疗多巴胺相关功能障碍，其中包括一个短暂但必要的“休息期”。在“休息期”期间，D1激动剂浓度降低，以获得亚最优激活D1多巴胺受体的激动剂血浆浓度，以防止耐受性的诱导。具体而言，该方法包括定期向患者施用半衰期为6小时左右的全D1激动剂，剂量导致第一血浆浓度的激动剂能够激活D1多巴胺受体以产生治疗效果。每24小时至少降低一次剂量，以获得第二较低的激动剂血浆浓度，该浓度能够在足够的时间内亚最优激活D1多巴胺受体，以防止耐受性的诱导。
• US6413977B1
  申请人：——

  公开号：US6413977B1

  公开（公告）日：2002-07-02
• US6916823B2
  申请人：——

  公开号：US6916823B2

  公开（公告）日：2005-07-12