Serotonin receptor (5-HT receptor) (5-HTR)

Serotonin receptors, or 5-hydroxytryptamine (5-HT) receptors, are a group of G protein-coupled receptors and one ligand-gated ion channel (5-HT3) that mediate the effects of the neurotransmitter serotonin (StatPearls, 2023). They are widely distributed in the central and peripheral nervous systems, where they regulate diverse functions such as mood, cognition, sleep, appetite, and gastrointestinal motility (NCBI, 2022). The family is divided into seven classes (5-HT1–5-HT7) based on their signaling mechanisms and structural properties (IUPHAR/BPS, 2023). These receptors are critical therapeutic targets; for instance, 5-HT1A partial agonists are used for anxiety, while 5-HT2A antagonists are key components of atypical antipsychotics (PubMed, 2021). Additionally, 5-HT3 antagonists are highly effective in treating nausea and vomiting associated with chemotherapy (NIH, 2023). Given their involvement in numerous physiological systems, drugs targeting specific 5-HT subtypes must be carefully designed to avoid off-target effects like serotonin syndrome or cardiac valvulopathy (FDA, 2020).

Other names

5-hydroxytryptamine receptor5-HT receptorSerotonin receptor family5-HTR

Drugs targeting the serotonin receptor family act through various mechanisms including agonism, antagonism, partial agonism, and inverse agonism across different subtypes (IUPHAR/BPS, 2023).