Chinese Academy of Sciences

Xiaohui Zhao

Ting Ting Zhang

Chen Chen

Gang Pei

Lixin Wei

Yanxiang Ni

Guoying Zhou

Jihong Tao

Huilan Yue

Wenjing Jia

The present invention relates to use of gTso thal in manufacturing a medicament for the promotion of MS-275 to cross the blood-brain barrier (BBB), and belongs to the technical field of pharmaceutical preparation. Administration of the medicament manufactured by the use of the present invention in combination with MS-275 significantly increases MS-275 to cross the BBB into the brain tissue, and prominently promotes the accumulation of MS-275 therein.

Use of gTso thal in manufacturing medicament for promotion of MS-275 to cross blood-brain barrier

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.

Screening G protein-coupled receptor antagonists for methods of treating Alzheimer's disease

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Shanghai, China

Xiaohui Zhao