Serotonin receptor family (5-HTR)

The Serotonin receptor family, also known as 5-hydroxytryptamine (5-HT) receptors, is a diverse group of receptors located throughout the central and peripheral nervous systems that mediate the physiological effects of serotonin (StatPearls, 2023). The family is classified into seven distinct classes (5-HT1 to 5-HT7) comprising 14 subtypes, most of which are G protein-coupled receptors, with the exception of the 5-HT3 receptor, which is a ligand-gated ion channel (IUPHAR/BPS Guide to Pharmacology). These receptors are integral to the regulation of mood, cognition, sleep, appetite, and gastrointestinal motility (UniProt). Dysregulation of serotonergic signaling is a hallmark of various conditions, including major depressive disorder, anxiety, schizophrenia, and migraine (PubMed, PMID: 28244281). Consequently, they are primary targets for a wide range of pharmacological agents, including antidepressants, antipsychotics, and antiemetics (PubChem). Therapeutic development focuses on subtype selectivity to maximize efficacy while minimizing risks such as serotonin syndrome or 5-HT2B-mediated cardiac valvulopathy (NIH).

Other names

5-hydroxytryptamine receptor5-HT receptorEnteramine receptor

Drugs act as agonists, partial agonists, antagonists, or inverse agonists at specific 5-HT receptor subtypes to modulate intracellular signaling pathways (e.g., cAMP, IP3/DAG) or gate ion flow in the case of 5-HT3 receptors (IUPHAR/BPS Guide to Pharmacology).