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

The Serotonin 5-hydroxytryptamine receptor 7 is a member of the G protein-coupled receptor superfamily activated by serotonin. It is encoded by the HTR7 gene in humans. The primary signaling mechanism involves coupling to stimulatory Gs proteins that activate adenylate cyclase, increasing intracellular cAMP levels. This leads to downstream activation of protein kinase A and other effectors involved in neuronal signaling. The receptor is widely expressed throughout the central nervous system—including thalamus, hypothalamus, hippocampus, cortex—and also found in peripheral tissues such as gastrointestinal tract smooth muscle and blood vessels. It plays key roles in regulating circadian rhythms/sleep-wake cycles, thermoregulation, learning/memory formation as well as neurodevelopmental processes like neurite outgrowth and synapse formation. Therapeutically it has become a focus for drug development aimed at treating depression—where blockade may enhance antidepressant actions—as well as cognitive dysfunction associated with psychiatric illnesses such as schizophrenia. Several atypical antipsychotics exhibit varying degrees of antagonistic activity at this site; lurasidone stands out for its high selectivity toward this target. There are multiple splice variants known which differ mainly at their carboxyl-terminal ends but share similar pharmacological properties except for differences affecting internalization rates. Overall modulation of this target offers promise not only for neuropsychiatric conditions but also potentially gastrointestinal pathologies where it mediates smooth muscle relaxation or pain sensitivity.

Other names

5-HT7 receptorHTR7Serotonin receptor 7

For drugs targeting this molecule, mechanisms include: – Antagonism at the 5‑HT₇ receptor to modulate neurotransmitter release and improve mood/cognition – Agonism or antagonism to alter cAMP signaling pathways in neurons and peripheral tissues