发明申请
- 专利标题: Methods of Identifying Improved NMDA Receptor Antagonists
- 专利标题(中): 识别改进的NMDA受体拮抗剂的方法
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申请号: US12772798申请日: 2010-05-03
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公开(公告)号: US20100272648A1公开(公告)日: 2010-10-28
- 发明人: Dennis C. Liotta , Raymond J. Dingledine , Stephen F. Traynelis
- 申请人: Dennis C. Liotta , Raymond J. Dingledine , Stephen F. Traynelis
- 主分类号: A61K49/00
- IPC分类号: A61K49/00 ; C12Q1/02
摘要:
Processes are provided for the identification a compound that is useful to treat or prevent a disorder that lowers the pH in a region of affected tissue comprising assessing the difference in potency, or potency boost, of the compound at physiological pH versus disorder-induced pH in a cell that expresses a human NMDA receptor. The assessment of potency boost can include measuring an IC50 of a compound at physiological pH and at disorder-induced pH (the “potency boost”) until a 95% confidence interval for the potency boost does not change more than 15% with the addition of a new experiment, wherein the measurements are repeated at least 5 times. The processes can be used for the selection of safe NMDA receptor antagonists for the treatment or prevention of a human disorder that lowers the pH in a region affected tissue. Such disorders include, but are not limited to, neuropathic pain, ischemic, Parkinsons disease, epilepsy and traumatic brain injuries.
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