5-HT2C
5-HT2C receptor is a subtype of 5-HT2 receptor that binds the endogenous neurotransmitter serotonin. It is a G protein-coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. HTR2C denotes the human gene encoding for the receptor, that is located on the X chromosome.
Function[edit | edit source]
The 5-HT2C receptor is known to regulate mood, anxiety, feeding, and reproductive behavior. In humans, the 5-HT2C receptor is established in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The 5-HT2C receptors control the release of dopamine and norepinephrine in areas such as the prefrontal cortex, nucleus accumbens, and striatum, thus playing a significant role in regulating the release of dopamine in these areas.
Ligands[edit | edit source]
Several ligands bind to the 5-HT2C receptor, including agonists, antagonists, and inverse agonists. Some of these ligands have therapeutic potential in treating disorders such as obesity, psychiatric disorders, sexual dysfunction, and incontinence.
Pharmacology[edit | edit source]
The 5-HT2C receptor is a target of many conventional and atypical antipsychotics. 5-HT2C receptors have a role in the therapeutic actions and side effects of these medications. Antagonism of 5-HT2C receptors by antipsychotic drugs can cause weight gain and insulin resistance.
Genetics[edit | edit source]
The HTR2C gene is located on the X chromosome. Mutations in this gene have been associated with Prader-Willi syndrome, mental retardation, and obesity.
See also[edit | edit source]
References[edit | edit source]
5-HT2C Resources | |
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Contributors: Prab R. Tumpati, MD