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Curr Opin Drug Discov Devel. 2008 Jul;11(4):438-45.

Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases.

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  • 1Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543, USA.


The serotonin 5-HT2C receptor is a G-protein-coupled receptor and is one of the 14 subtypes that constitutes the serotonin receptor family. Agonists of 5-HT2C have been implicated as potential treatments for diseases of significant unmet medical need, including obesity and schizophrenia. Despite approximately 10 years of discovery efforts, 5-HT2C agonists have only recently advanced into the clinic, likely because many of the early drug discovery efforts experienced significant difficulties with attaining receptor selectivity. Several of these issues related to receptor selectivity have now been overcome, resulting in the entry of compounds into advanced clinical trials. This review summarizes the progress in 5-HT2C agonist discovery and clinical development over the last 3 years. [sw1]what are the several issues - several issues relating to receptor selectivity?

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