5-HT4 receptor

5-HT4 receptor is a type of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-hydroxytryptamine (5-HT). The 5-HT4 receptor is a member of the G protein-coupled receptor (GPCR) family. It is coupled to the G protein Gs, which activates an intracellular second messenger cascade to produce an excitatory response in neurons.

Function

The 5-HT4 receptor is located in the gastrointestinal tract, urinary bladder, heart and adrenal gland, as well as in the central nervous system. In the gastrointestinal tract, it is involved in the regulation of gastrointestinal motility. In the brain, it is involved in the modulation of neurotransmitter release, and may be involved in the therapeutic effects of antidepressants and antipsychotics.

Pharmacology

Several drugs act as agonists or antagonists at the 5-HT4 receptor, including the antidepressants prucalopride, tegaserod and cisapride. These drugs have been used for the treatment of irritable bowel syndrome, gastroesophageal reflux disease (GERD), and constipation.

Clinical significance

Alterations in 5-HT4 receptor function have been implicated in depression, anxiety, schizophrenia, and Parkinson's disease. Research is ongoing to develop new drugs that target the 5-HT4 receptor for the treatment of these and other conditions.

See also

• 5-HT receptor
• Serotonin
• G protein-coupled receptor
• Neurotransmitter
• Antidepressant
• Antipsychotic

References

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