1221408-00-9Relevant articles and documents
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents
Ahmad, Saleem,Ngu, Khehyong,Miller, Keith J.,Wu, Ginger,Hung, Chen-pin,Malmstrom, Sarah,Zhang, Ge,O'Tanyi, Eva,Keim, William J.,Cullen, Mary Jane,Rohrbach, Kenneth W.,Thomas, Michael,Ung, Thao,Qu, Qinling,Gan, Jinping,Narayanan, Rangaraj,Pelleymounter, Mary Ann,Robl, Jeffrey A.
scheme or table, p. 1128 - 1133 (2010/06/15)
Agonists of the 5-HT2C receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT2B receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor is described. Among these, compounds (+)-2a and (+)-3c were identified as potent and highly selective agonists which exhibited weight loss in a rat model upon oral dosing.
