Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT 2C receptor agonists

G Zhao, C Kwon, SN Bisaha, PD Stein, KA Rossi…

Index: Zhao, Guohua; Kwon, Chet; Bisaha, Sharon N.; Stein, Philip D.; Rossi, Karen A.; Cao, Xueying; Ung, Thao; Wu, Ginger; Hung, Chen-Pin; Malmstrom, Sarah E.; Zhang, Ge; Qu, Qinling; Gan, Jinping; Keim, William J.; Cullen, Mary Jane; Rohrbach, Kenneth W.; Devenny, James; Pelleymounter, Mary Ann; Miller, Keith J.; Robl, Jeffrey A. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 13 p. 3914 - 3919

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Citation Number: 3

Abstract

The 5-HT2C receptor has been implicated as a critical regulator of appetite. Small molecule activation of the 5-HT2C receptor has been shown to affect food intake and regulate body weight gain in rodent models and more recently in human clinical trials. Therefore, 5- ...