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Identification of N-Propylnoraporphin-11-yl 5-(1,2-Dithiolan-3-yl)pentanoate as a New Anti-Parkinson's Agent Possessing a Dopamine D-2 and Serotonin 5-HT1A Dual-Agonist Profile

文献类型：期刊论文

作者Zhang, Hai1; Ye, Na2; Zhou, Shanglin3; Guo, Lin3; Zheng, Longtai1; Liu, Zhili2; Gao, Bo1; Zhen, Xuechu1,3; Zhang, Ao2
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2011-07-14
卷号54期号:13页码:4324-4338
ISSN号0022-2623
DOI10.1021/jm200347t
文献子类Article
英文摘要A series of new aporphine analogues (aporlogues) were synthesized bearing a C-, N-, or O-linkage at the C11 position. Lipoic ester (-)-15 was identified as a full agonist at the dopamine D-2 and serotonin 5-HT1A receptors with K-i values of 174 and 66 nM, respectively. It elicited antiparkinsonian action on Parkinsin's disease (PD) rats with minor dyskinesia. Chronic use of (-)-15 reduced L-DOPA-induced dyskinesia (LID) without attenuating the antiparkinsonian effect. These results suggest that 5-HT1A and D-2 dual-receptor agonist (-)-15 may present a novel candidate drug in the treatment of PD and LID.
WOS关键词DOPA-INDUCED DYSKINESIA ; ALPHA-LIPOIC ACID ; RECEPTOR STIMULATION ; FUTURE-DIRECTIONS ; FOSB EXPRESSION ; RAT MODEL ; DISEASE ; PHARMACOLOGY ; ANTIOXIDANT ; SARIZOTAN
资助项目Chinese National Science Foundation[30772625] ; Chinese National Science Foundation[81072528] ; Chinese National Science Foundation[30825042] ; Ministry of Science and Technology of China[2009CB522000] ; Shanghai Commission of Science and Technology[10410702600] ; Shanghai Commission of Science and Technology[10JC1417100] ; Shanghai Commission of Science and Technology[10dz1910104] ; National Science and Technology Major Project on "Key New Drug Creation and Manufacturing Program"[2009ZX09301-001] ; National Science and Technology Major Project on "Key New Drug Creation and Manufacturing Program"[2009ZX09103-062] ; National Science and Technology Major Project on "Key New Drug Creation and Manufacturing Program"[2009ZX09102]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000292479600003
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/278475]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
药理学第二研究室
通讯作者Zhen, Xuechu
作者单位1.Soochow Univ, Coll Pharmaceut Sci, Dept Pharmacol, Suzhou 215325, Peoples R China;
2.Chinese Acad Sci, SOMCL, SIMM, Shanghai 201203, Peoples R China;
3.Chinese Acad Sci, State Key Lab Drug Res, SIMM, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Hai,Ye, Na,Zhou, Shanglin,et al. Identification of N-Propylnoraporphin-11-yl 5-(1,2-Dithiolan-3-yl)pentanoate as a New Anti-Parkinson's Agent Possessing a Dopamine D-2 and Serotonin 5-HT1A Dual-Agonist Profile[J]. JOURNAL OF MEDICINAL CHEMISTRY,2011,54(13):4324-4338.
APA Zhang, Hai.,Ye, Na.,Zhou, Shanglin.,Guo, Lin.,Zheng, Longtai.,...&Zhang, Ao.(2011).Identification of N-Propylnoraporphin-11-yl 5-(1,2-Dithiolan-3-yl)pentanoate as a New Anti-Parkinson's Agent Possessing a Dopamine D-2 and Serotonin 5-HT1A Dual-Agonist Profile.JOURNAL OF MEDICINAL CHEMISTRY,54(13),4324-4338.
MLA Zhang, Hai,et al."Identification of N-Propylnoraporphin-11-yl 5-(1,2-Dithiolan-3-yl)pentanoate as a New Anti-Parkinson's Agent Possessing a Dopamine D-2 and Serotonin 5-HT1A Dual-Agonist Profile".JOURNAL OF MEDICINAL CHEMISTRY 54.13(2011):4324-4338.

入库方式： OAI收割

来源：上海药物研究所

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