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Bioorg Med Chem Lett. 2010 Feb 1;20(3):1128-33. doi: 10.1016/j.bmcl.2009.12.014. Epub 2009 Dec 6.

Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.

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Research & Development, Bristol-Myers Squibb Co, PO Box 4000, Princeton, NJ 08543, United States.


Agonists of the 5-HT(2C) 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-HT(2B) receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT(2C) agonists with no detectable agonism of the 5-HT(2B) 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.

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