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.