5-hydroxytryptamine receptor 7 (5-HT7 receptor) (5-HT7R)

The 5-hydroxytryptamine receptor 7 (5-HT7 receptor) is a member of the G protein-coupled receptor (GPCR) superfamily and is the most recently identified serotonin receptor (UniProt: P34969). It is primarily coupled to the Gs protein, which stimulates adenylyl cyclase and increases intracellular cAMP levels (IUPHAR/BPS Guide to Pharmacology). In humans, the HTR7 gene undergoes alternative splicing to produce three functional isoforms—5-HT7(a), 5-HT7(b), and 5-HT7(d)—which differ in their C-terminal sequences but exhibit similar pharmacological properties (Guseva et al., 2014). The receptor is widely expressed in the central nervous system, particularly in the hypothalamus, thalamus, and hippocampus, where it regulates circadian rhythms, thermoregulation, and cognitive processes (PubMed: 24333168). It is also found in the periphery, mediating smooth muscle relaxation in the gastrointestinal tract and blood vessels (Hedlund, 2009). The 5-HT7 receptor is a significant therapeutic target for psychiatric and neurological disorders, including major depressive disorder, anxiety, and cognitive deficits in schizophrenia. Several atypical antipsychotics and antidepressants, such as lurasidone and vortioxetine, act as potent antagonists at this receptor, contributing to their clinical profile (NCBI Gene: 3363).

Other names

Serotonin receptor 7HTR75-HT75-hydroxytryptamine receptor 7 isoform a5-hydroxytryptamine receptor 7 isoform b5-hydroxytryptamine receptor 7 isoform d

Antagonism or agonism of the Gs-coupled signaling pathway to modulate intracellular cAMP levels and downstream neuronal excitability.