5-hydroxytryptamine receptor 3B-containing heteromeric receptor (5-HT3AB receptor)

The 5-HT3B-containing 5-HT3 receptor is a heteromeric ligand-gated ion channel composed of 5-HT3A and 5-HT3B subunits. While the 5-HT3A subunit can form functional homomeric receptors, the 5-HT3B subunit must heteromerize with 5-HT3A to reach the cell surface and alter the biophysical properties of the channel, significantly increasing single-channel conductance and decreasing calcium permeability (PubMed: 10353249, UniProt: O95264). These receptors are primarily expressed in the central and peripheral nervous systems, where they mediate fast excitatory neurotransmission and play a critical role in the emetic reflex and gastrointestinal motility (StatPearls: NBK554513). In clinical practice, these receptors are the primary targets for 'setron' class drugs used to manage chemotherapy-induced and postoperative nausea and vomiting. Genetic variations in the HTR3B gene have been linked to differences in individual responses to antiemetic therapy and susceptibility to psychiatric conditions such as alcohol dependence and major depression (PubMed: 15555062).

Other names

5-HT3B receptor subunitSerotonin receptor 3BHTR3B5-hydroxytryptamine receptor subunit 3BHeteromeric 5-HT3 receptor

Antagonism of the 5-HT3 receptor complex, which inhibits the opening of the non-selective cation channel, thereby preventing serotonin-mediated depolarization of peripheral and central neurons.