New 5-HT2C receptor agonists

Abstract

While there is evidence for the involvement of different serotonin (5hydroxytryptamine; 5-HT) receptors in the regulation of food intake and body weight maintenance, the data supporting the role of the 5-HT_2C receptor are especially strong. This information has elevated 5-HT_2C receptor activation into one of the most competitive research areas for antiobesity therapy, a therapeutic area with few (if any) safe, effective pharmacological agents available. Varying amounts of evidence also exist to support the use of 5-HT_2C agonists for the pharmacological treatment of several other conditions, including anxiety, depression, obsessive–compulsive disorder, sexual dysfunction, epilepsy, urinary incontinence and hot flushes. The therapeutic potential of 5-HT_2C receptor modulation has spawned a successful search for 5-HT_2C receptor agonists. This review will focus on recent patent applications through August 2003 that describe compounds that have agonist activity at the 5-HT_2C receptor, and should be complementary to previous Expert Opinion discussions on the 5-HT_2C receptor [1-7].

• 5-hydroxytryptamine (5-HT)
• 5-HT2C agonist
• 5-HT2C receptor
• Alzheimer’s disease
• anxiety
• depression
• epilepsy
• G-protein-coupled receptor
• hot flushes
• obesity
• obsessivecompulsive disorder (OCD)
• serotonin
• sexual dysfunction
• urinary incontinence