The 5-HT3 receptors are the only serotonergic receptors belonging to ligand-gated ion channel superfamily. Particularly, these membrane-spanning ‘cationotropic’ receptors belong to a pentameric neurotransmitter-gated Cys-loop receptor class and are responsible for fast excitatory and inhibitory neurotransmission. Until now, five subtypes of 5HT3Rs have been identified in humans; HTR3A, a homopentameric type and HTR3B, a heteropentameric form, and HTR3D, HTR3E, HTR3F that are yet to be elucidated. It is reported that 5-HT3Rs are widely distributed in different regions of the brain in rodents, primates, and humans, in particular, those that regulate affective behavior. Studies have shown that ionotropic 5HT3Rs could mediate fast neuronal transmission and subsequent neuromodulation in discrete brain areas. Stimulation of 5HT3Rs results in channel opening and the influx of cations into the cell, leading to rapid membrane depolarization and release of neurotransmitters. What’s more, several studies have reported that antagonism of 5HT3Rs produces antidepressant-like effects, indicating 5HT3Rs may act as a potential target for antidepressants
Here, we give a comprehensive introduction of members of the 5-HT3 receptor family, such as 5-hydroxytryptamine receptor 3A, 5-hydroxytryptamine receptor 3B, and 5-hydroxytryptamine receptor 3C. To learn more detailed information, please click the links below.
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