Serotonin 5-HT2C and 5-HT2B receptors (5-HT2C/5-HT2B receptors)

The Serotonin 5-hydroxytryptamine receptor 2C (5-HT2C) and 2B (5-HT2B) are class A G protein-coupled receptors activated by the endogenous neurotransmitter serotonin. Both are important for excitatory neurotransmission, but differ in tissue distribution and physiological roles. 5-HT2C is predominantly found in the central nervous system, especially the choroid plexus and regions regulating mood, appetite, and dopamine signaling. Its function is modulated by RNA editing, which affects activity and drug response[2]. 5-HT2B is more prominent in peripheral organs, especially the heart and gastrointestinal tract, regulating cardiovascular function, cell proliferation, and fibrotic responses[3]. Both receptors are major drug targets for psychiatric, metabolic, and cardiovascular therapeutics. Safety concerns mean drug selectivity is essential, particularly to avoid 5-HT2B-mediated cardiac side effects.

Other names

5-HT2C receptorHTR2Cserotonin receptor 2Chydroxytryptamine receptor 2C5-HT2B receptorHTR2Bserotonin receptor 2Bhydroxytryptamine receptor 2B

Agonists activate the receptor (e.g., lorcaserin promotes satiety via 5-HT2C). Antagonists block the receptor—used for research in obesity, neuropsychiatric disorders, and cardiovascular risks (e.g., ritanserin for 5-HT2C). Inverse agonists reduce constitutive receptor activity (e.g., ritanserin on 5-HT2C). Biased signaling (especially for novel 5-HT2B antagonists). Modulation of dopamine release, impacting mood and behavior.