Pharmacophore comparison and development of recently discovered long chain arylpiperazine and sulfonamide based 5-HT7 ligands
Mini-Reviews in Medicinal Chemistry
5-HT7, Arylpiperazine, CNS, Drug design, Pharmacophore, Serotonin
The serotonin system exerts its effects on the CNS and many peripheral systems. Of the 14 serotonin receptors, the 5-HT7 receptor is the most recently discovered. The 5-HT7 receptor has been shown to be involved in stress reduction, depression, and nociceptive control. Despite the 20 years since the discovery of 5-HT7R, there are still few truly selective ligands. Two of the common scaffolds for 5-HT7R ligands are long chain arylpiperazines (LCAPs) and sulfonamide containing compounds. This review focuses on recently developed (2014-2016) 5-HT7R ligands, their selectivity for the receptor, and suggests the possible new pharmacophore models for these ligands.
Rague, A., & Tidgewell, K. (2018). Pharmacophore comparison and development of recently discovered long chain arylpiperazine and sulfonamide based 5-HT7 ligands. Mini-Reviews in Medicinal Chemistry, 18 (7), 552-560. https://doi.org/10.2174/1389557517666170913111533