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发现强效孤儿G蛋白偶联受体88(GPR88)激动剂,用于中枢神经系统疾病的潜在治疗。

The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.

作者信息

Bi Yingzhi, Dzierba Carolyn D, Fink Cynthia, Garcia Yudith, Green Michael, Han Jianxin, Kwon Soojin, Kumi Godwin, Liang Zhi, Liu Ying, Qiao Ying, Zhang Yulian, Zipp Greg, Burford Neil, Ferrante Meredith, Bertekap Robert, Lewis Martin, Cacace Angela, Westphal Ryan S, Kimball David, Bronson Joanne J, Macor John E

机构信息

Lexicon Pharmaceuticals, Inc., 350 Carter Road, Princeton, NJ 08540, United States.

Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, United States.

出版信息

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1443-7. doi: 10.1016/j.bmcl.2015.02.038. Epub 2015 Feb 21.

Abstract

Modulating GPR88 activity is suggested to have therapeutic utility in the treatment of CNS disorders, such as schizophrenia. This Letter will describe the discovery and SAR development of a class of potent GPR88 agonists.

摘要

调节GPR88活性被认为在治疗中枢神经系统疾病(如精神分裂症)方面具有治疗效用。本信函将描述一类强效GPR88激动剂的发现和构效关系研究进展。

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