5-Hydroxytryptamine 3 Receptor (5-HT3)

The 5-hydroxytryptamine 3 receptor (5-HT3) is a member of the serotonin receptor family that functions as a ligand-gated ion channel. It mediates fast excitatory neurotransmission in both the central and peripheral nervous systems by allowing cation influx upon activation, leading to neuronal depolarization and excitation. The functional 5-HT3 receptor is a pentameric complex consisting of five subunits arranged around a central pore. Activation leads to rapid cation influx—primarily Na+, K+, and Ca2+—causing neuronal excitation. Antagonists targeting this receptor class (setrons) are clinically important antiemetics. Genetic polymorphisms in genes encoding 5-HT3 subunits can affect expression levels or function of receptors, influencing disease susceptibility or drug response profiles.

Other names

Serotonin 3 receptor5-HT3 receptor

Antagonism of 5-HT3 receptor, blocking cation influx and reducing neuronal excitation.