5-Hydroxytryptamine receptor (5-HTR) (5-HTR)

The 5-Hydroxytryptamine (5-HT) receptor family, commonly known as serotonin receptors, consists of a diverse group of proteins that mediate the physiological effects of the neurotransmitter serotonin in the central and peripheral nervous systems (StatPearls: Serotonin Receptors). These receptors are classified into seven distinct families (5-HT1 to 5-HT7), comprising at least 14 subtypes; all are G protein-coupled receptors except for the 5-HT3 receptor, which is a ligand-gated ion channel (IUPHAR/BPS Guide to Pharmacology). They play critical roles in regulating a wide array of biological processes, including mood, sleep, appetite, cognition, and vascular tone. In clinical practice, multiple 5-HT receptor subtypes are often targeted simultaneously by drugs to treat complex conditions such as schizophrenia, depression, and migraine (NCBI: Serotonin Receptors). For example, atypical antipsychotics often combine 5-HT2A antagonism with dopamine receptor modulation, while triptans act as agonists at 5-HT1B and 5-HT1D receptors. However, non-selective modulation of these receptors can lead to significant safety concerns, most notably serotonin syndrome, a potentially life-threatening condition resulting from excessive serotonergic activity. Additionally, certain subtypes like 5-HT2B are associated with specific risks such as cardiac valvulopathy when chronically activated.

Other names

Serotonin receptor5-HT receptor5-hydroxytryptamine receptor family

Drugs targeting multiple 5-HT receptor subtypes typically act through agonism, antagonism, or partial agonism to modulate intracellular signaling pathways (e.g., cAMP or IP3/DAG) or ion conductance, thereby influencing neuronal excitability and neurotransmitter release.