发明名称 Methods of Identifying Improved NMDA Receptor Antagonists
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.
申请公布号 US2010272648(A1) 申请公布日期 2010.10.28
申请号 US20100772798 申请日期 2010.05.03
申请人 LIOTTA DENNIS C;DINGLEDINE RAYMOND J;TRAYNELIS STEPHEN F 发明人 LIOTTA DENNIS C.;DINGLEDINE RAYMOND J.;TRAYNELIS STEPHEN F.
分类号 A61K49/00;C12Q1/02 主分类号 A61K49/00
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