5-HT1B

5-HT1B receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin. It is a G protein-coupled receptor (GPCR) that is coupled to Gi/Go and inhibits adenylyl cyclase. This receptor is predominantly found in the human brain, particularly in the substantia nigra, the striatum and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. Autoreceptors are located on serotonin-releasing neurons and function as a part of a negative feedback loop, whereas heteroreceptors are located on the target neurons of serotonin-releasing neurons.

Function

The 5-HT1B receptors are found in various parts of the brain with the highest concentrations in the basal ganglia, hippocampus, cortex, and frontal lobe. They are less densely populated in the cerebellum and thalamus, and are found in low amounts in the pons and periaqueductal gray.

Clinical significance

The 5-HT1B receptor is suspected to have a role in several disorders including depression, obsessive-compulsive disorder, eating disorders, migraine, and substance abuse. It is also considered a target for the treatment of schizophrenia and Parkinson's disease.

Ligands

Several selective 5-HT1B agonists have been developed, including CP-93,129, Anpirtoline, and Zolmitriptan. Antagonists include SB-216641, NAS-181, and Isamoltane.

See also

• 5-HT receptor
• Serotonin
• G protein-coupled receptor

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