公开(公告)号：US20080312332A1

公开(公告)日：2008-12-18

申请号：US12159183

申请日：2006-12-26

申请人： Gang Pei ,  Yanxiang Ni ,  Xiaohui Zhao

发明人： Gang Pei ,  Yanxiang Ni ,  Xiaohui Zhao

IPC分类号： A61K31/138 ,  G01N33/566 ,  A61P25/28

CPC分类号： G01N33/5035 ,  G01N2333/726 ,  G01N2500/10 ,  G01N2800/2821

摘要： A method for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. Uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis.

摘要翻译： 用于筛选用于治疗或预防阿尔茨海默病或相关神经病理学的试剂的方法包括以下步骤：（a）激活受体并测定受体的第一内吞程度，其中所述受体是G蛋白偶联受体， 与早老素-1; （b）在与候选试剂的存在下在与步骤（a）相同的条件下活化受体，并确定受体的第二程度的胞吞作用; （c）确定第一内吞程度与第二内吞程度之间的差异; 和（d）如果差值小于阈值，则重复步骤（a） - （c）。 用于制备用于治疗或预防阿尔茨海默病或相关神经病理学的药物的受体拮抗剂的用途，其中所述受体拮抗剂抑制内吞作用期间与早老蛋白-1相关的G蛋白偶联受体的内吞。