SEROTONIN 5-HT2C RECEPTOR AGONISTS: POTENTIAL FOR THE TREATMENT OF OBESITY
Mol. Interv. 2005 5: 282-291.
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By the mid to late 1990s, the anorectic drug fenfluramine was prescribed to millions of patients annually, until the FDA announced withdrawal of the drug in 1997. Today, the epidemic of obesity calls ever more compellingly for new pharmacological therapeutics. But will it be possible to activate serotoninergic signaling in the brain (as did fenfluramine) without compromising cardiovascular health (as did fenfluramine)? One possibility for the selective targeting of obesity may be the serotonin 5-HT2C receptor, which appears to be associated with the signaling of satiety in energy-regulating centers in the brain. There are indications that selective activation of serotonin receptor subtypes may be possible, albeit difficult, and a variety compounds are under investigation in an effort to do so in the clinic.