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Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin 1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline
Wang, Dong1; Yang, Liguo1; Su, Jingjing1; Niu, Yan2; Lei, Xiaoping2; Xiong, Juan3; Cao, Xiaohua1; Hu, Yinghe1; Mei, Bing1; Hu, Jin-Feng1,3
关键词Xanomeline EUK1001 Muscarinic M1 agonist Presenilins Neurodegeneration Alzheimer&prime s disease
刊名BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
2011-07-01
DOI10.1016/j.bbrc.2011.05.120
410期:2页:229-234
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Biophysics
研究领域[WOS]Biochemistry & Molecular Biology ; Biophysics
关键词[WOS]MUSCARINIC RECEPTOR AGONIST ; INFLAMMATORY RESPONSES ; BEHAVIORAL SYMPTOMS ; AGED MICE ; OUT MICE ; DISEASE ; MEMORY ; ENHANCEMENT ; DEFICITS ; IMPROVES
英文摘要

The M1/M4-preferring muscarinic agonist xanomeline was found to have some benefit in the treatment of the memory impairment of Alzheimer′s disease (AD), but side effects precluded further development. EUK1001, a fluorinated derivative of xanomeline, because of greater affinity for M1 muscarinic receptors, is likely to have a significantly better side effect profile than xanomeline. We have now studied the effects of 3-month chronic administration of EUK1001 and xanomeline (0.5 mg/kg/day) in AD-like presenilin 1/presenilin 2 conditional double knockout (PS cDKO) mice. Only EUK1001 was found to significantly ameliorate the deficit in recognition memory. Histological analysis demonstrated partial attenuation of the brain atrophy in EUK1001-treated PS cDKO mice and minimal effect in the xanomeline-treated mice. Both compounds effectively suppressed the elevation of brain tau phosphorylation in the PS cDKO mice, but neither inhibited the increased inflammatory responses. These results indicate that EUK1001 showed superiority to xanomeline with regard to attenuation of several AD-like neurodegenerative phenotypes in PS cDKO mice. These results suggest further investigation of the development of EUK1001 for the treatment of AD is indicated. (C) 2011 Elsevier Inc. All rights reserved.

语种英语
WOS记录号WOS:000292623800013
项目编号90713040 ; 30640068 ; 81070876 ; 31070993 ; 07DZ22006 ; 06DZ19002 ; 06PJ14033
资助机构NSFC ; STCSM
引用统计
被引频次:14[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/64114
专题北京大学药学院
作者单位1.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China
2.E China Normal Univ, Shanghai Key Lab Brain Funct Genom MOE & SBFG, Minist Educ, Key Lab Brain Funct Genom, Shanghai 200062, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
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GB/T 7714
Wang, Dong,Yang, Liguo,Su, Jingjing,et al. Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin 1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2011,410(2):229-234.
APA Wang, Dong.,Yang, Liguo.,Su, Jingjing.,Niu, Yan.,Lei, Xiaoping.,...&Hu, Jin-Feng.(2011).Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin 1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,410(2),229-234.
MLA Wang, Dong,et al."Attenuation of neurodegenerative phenotypes in Alzheimer-like presenilin 1/presenilin 2 conditional double knockout mice by EUK1001, a promising derivative of xanomeline".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 410.2(2011):229-234.
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