Importance of the field: The 5-HT(2C) receptor is a GPCR and is one of the 14 subtypes that constitute the serotonin receptor family. The 5-HT₂(C) receptor is exclusively expressed in the CNS where it demonstrates a wide distribution and displays high-affinity interactions with a wide variety of psychiatric medications. Modulators of 5-HT₂(C) have been implicated as a potential treatment for diseases of significant unmet medical need, including obesity, schizophrenia, depression, anxiety, Parkinson's disease, drug addiction, erectile dysfunction and urinary incontinence. Thus, there is a great interest in developing potent and selective 5-HT₂(C) receptor modulators.
Areas covered in this review: This review article highlights the research progress in 5-HT₂(C) receptor modulators published in the patent literature between January 2003 and June 2010, giving emphasis to the medicinal chemist's standpoint.
What the reader will gain: Readers will rapidly gain an overview of the various 5-HT₂(C) receptor modulators reported in the patent literature in the past 8 years. Furthermore, the readers will learn which structure type can interact with the 5-HT₂(C) receptor. In addition, the readers will be aware of the pharmaceutical companies that have been the main players in the field.
Take home message: There is substantial evidence supporting the concept that a selective 5-HT₂(C) receptor modulator should provide benefit in the treatment of a variety of CNS disorders. Although research efforts have identified several promising 5-HT₂(C) receptor modulators that display high functional selectivity, further clinical efficacy and safety data are needed to prove their actual clinical utility. Therefore, the query for selectively acting 5-HT₂(C) receptor modulators is still ongoing.