Zonampanel monohydrate | 466685-98-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Zonampanel monohydrate
• 英文别名: 2-(7-imidazol-1-yl-6-nitro-2,3-dioxo-4H-quinoxalin-1-yl)acetic acid;hydrate
• CAS: 466685-98-3
• 化学式: C13H11N5O7
• 分子量: 349.26
• InChiKey: OBHWTRBRRFQGRJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.96
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  151
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• New use of glutamate antagonists for the treatment of cancer
  申请人：Ikonomidou, Hrissanthi

  公开号：EP1002535A1

  公开（公告）日：2000-05-24

  New therapies can be devised based upon a demonstration of the role of glutamate in the pathogenesis of cancer. Inhibitors of the interaction of glutamate with the AMPA, kainate, or NMDA receptor complexes are likely to be useful in treating cancer and can be formulated as pharmaceutical compositions. They can be identified by appropriate screens.

  根据谷氨酸在癌症发病机制中的作用，可以设计出新的疗法。谷氨酸与 AMPA、kainate 或 NMDA 受体复合物相互作用的抑制剂可能有助于治疗癌症，并可配制成药物组合物。它们可以通过适当的筛选来确定。
• Composition for the treatment of ischemic stroke containing zonampanel and a tissue plasminogen activator
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1316313A2

  公开（公告）日：2003-06-04

  The present invention relates to a combination of [7-(1H-imidazol-1-yl)-6-nitro-2, 3-dioxo-3, 4-dihydroquinoxalin-1(2H)-yl]acetic acid or a salt or hydrate thereof or, preferably, zonampanel together with a tissue plasminogen activator for the therapy of ischemic stroke or for the improvement of neurological symptom accompanied by cerebral infarction, to a method of administration thereof and to a method of therapy therefor. The combination of the present invention showed better effect of reducing the infarct volume than administration of a single component. Therefore, the combination of the present invention is useful as a therapy for ischemic stroke.

  本发明涉及一种[7-(1H-咪唑-1-基)-6-硝基-2，3-二氧代-3，4-二氢喹喔啉-1(2H)-基]乙酸或其盐或水合物的组合物，或优选唑南帕尼与组织纤溶酶原激活剂的组合物，用于治疗缺血性中风或改善伴随脑梗塞的神经症状，并涉及其给药方法和治疗方法。与服用单一成分相比，本发明的组合物在减少梗塞体积方面显示出更好的效果。 因此，本发明的组合物可用于缺血性中风的治疗。
• THERAPEUTIC AGENT FOR BRAIN HEMORRHAGE
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1518556A1

  公开（公告）日：2005-03-30

  It was found that an AMPA receptor antagonist zonampanel or a salt or the like thereof has an effect to improve cerebral hemorrhage and neurological symptoms accompanied by cerebral hemorrhage and therefore is useful as an agent for treating cerebral hemorrhage.

  研究发现，AMPA 受体拮抗剂佐南帕奈或其盐或类似物具有改善脑出血和脑出血伴随的神经症状的作用，因此可作为治疗脑出血的药物。
• INHIBITION OF PROLIFERATION AND INFILTRATION OF BRAIN TUMOR CELLS CAUSED BY EXPRESSION OF AMPA-TYPE GLUTAMATE RECEPTOR SUBUNIT
  申请人：Japan Science and Technology Agency

  公开号：EP1552852A1

  公开（公告）日：2005-07-13

  The present invention is to provide a method of treatment which inhibits proliferation and invasion of brain tumor cells in developing animal brain tumor cells, and a method for measuring proliferation/invasion activity of brain tumor cells, in the brain tumor cells, preferably, in glioblastoma. Proliferation and invasion of brain tumor cells are inhibited by regulating Ca2+ permeability by glutamate receptor subunits in developing animal brain tumor cells. Regulation of Ca2+ permeability by glutamate receptor subunits can be conducted by introducing the GluR2 gene into AMPA-type glutamate receptors in brain tumor cells. Further, the present invention provides a method for measuring proliferation/invasion activity of brain tumor cells by detecting/measuring the expression of glutamate receptor subunits in developing animal brain tumor cells.

  本发明旨在提供一种在发育中的动物脑肿瘤细胞中抑制脑肿瘤细胞增殖和侵袭的治疗方法，以及一种测量脑肿瘤细胞（最好是胶质母细胞瘤）增殖/侵袭活性的方法。通过调节发育中动物脑肿瘤细胞中谷氨酸受体亚基对 Ca2+ 的通透性，可抑制脑肿瘤细胞的增殖和侵袭。谷氨酸受体亚基对 Ca2+ 通透性的调节可通过将 GluR2 基因导入脑肿瘤细胞中的 AMPA 型谷氨酸受体来实现。此外，本发明还提供了一种通过检测/测量发育中动物脑肿瘤细胞中谷氨酸受体亚基的表达来测量脑肿瘤细胞增殖/侵袭活性的方法。
• PROBENECID FOR USE IN TREATING EPILEPTIC DISEASES, DISORDERS OR CONDITIONS
  申请人：Paris Sciences et Lettres - Quartier Latin

  公开号：EP3427729A1

  公开（公告）日：2019-01-16

  The present invention relates to probenecid or a pharmaceutical acceptable salt thereof for use in the treatment of a neurological disorder in a subject in need thereof, wherein administration of probenecid or a pharmaceutical acceptable salt thereof inhibits compulsive behaviors or electrographic seizures in said subject. Preferably, said neurological disorder is an epileptic disease, disorder or condition.

  本发明涉及丙磺舒或其药物可接受盐，用于治疗有需要的受试者的神经系统疾病，其中服用丙磺舒或其药物可接受盐可抑制所述受试者的强迫行为或电图癫痫发作。优选地，所述神经紊乱是癫痫疾病、紊乱或病症。