Serotonin receptor 2B and 2C (5-HT2B and 5-HT2C)

Serotonin receptor 2B (5-HT2B) and serotonin receptor 2C (5-HT2C) are closely related G protein-coupled receptors (GPCRs) that bind serotonin (5-hydroxytryptamine). Both are part of the 5-HT2 receptor family, but have distinct genetic, anatomical, and functional profiles. The 5-HT2B receptor plays a significant peripheral role, especially in the heart, where overstimulation can lead to cardiac valvulopathy. The 5-HT2C receptor is primarily expressed in the brain and influences mood, feeding, and neuroendocrine regulation. Aberrant activity of these receptors contributes to cardiovascular, neurological, and psychiatric diseases. Many drugs interact with one or both receptors, with clinical relevance ranging from obesity treatment (2C agonists) to cardiovascular risk (2B agonists)[1][2][3][4][5][7].

Other names

5-HT2B receptor5-HT2C receptor5-hydroxytryptamine receptor 2B5-hydroxytryptamine receptor 2CHTR2B (gene for 2B)HTR2C (gene for 2C)Serotonin receptor B/C (rare, nonstandard)5-HT2B/2C (composite, nonstandard)

Agonists promote downstream Gq/11 signaling, leading to phospholipase C activation and increased intracellular calcium Antagonists/inverse agonists block receptor activity and downstream signaling Some drugs (e.g., fenfluramine) overstimulate 2B, leading to cardiac fibroblast proliferation and valvulopathy[1][5] Agonism at 2C reduces appetite via CNS-mediated mechanisms (e.g., lorcaserin)[2]