Topic summary
5-HT3 receptor
The 5-HT3 receptors are a subclass of serotonin (5-HT) receptors. They belong to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and differ structurally and functionally from all other serotonin receptors, which are G protein-coupled receptors. 5-HT3 receptors are cation channels, that is, they are permeable to sodium (Na), potassium (K), and calcium (Ca) ions and mediate neuronal depolarization and excitation within the central and peripheralnervous systems.
As with other ligand gated ion channels, the 5-HT3 receptor consists of five subunits arranged around a central ion conducting pore. Binding of the neurotransmitter serotonin (or 5-hydroxytryptamine) to the 5-HT3 receptor opens the channel, which, in turn, leads to an excitatory response in neurons. The rapidly activating, desensitizing, inward current is predominantly carried by sodium and potassium ions. 5-HT3 receptors have a negligible permeability to anions. They are most closely related by homology to the nicotinic acetylcholine receptor.