Serotonin 5-hydroxytryptamine receptor 2A (5-HT2A) and serotonin 5-hydroxytryptamine receptor 2C (5-HT2C) (5-HT2A, 5-HT2C)

Serotonin 5-hydroxytryptamine receptor 2A (5-HT2A) and 5-hydroxytryptamine receptor 2C (5-HT2C) are closely related members of the G protein-coupled receptor (GPCR) family, primarily expressed in the central nervous system and responsible for mediating the effects of the neurotransmitter serotonin[1][2][5]. These receptors share structural similarities, including seven transmembrane helices, and primarily couple to the Gq/11 family of G proteins, activating phospholipase C and downstream signal transduction pathways[1][2]. They play crucial roles in cognition, perception, mood regulation, and several physiological and pathophysiological processes ranging from psychiatric disease (depression, schizophrenia, psychosis) to metabolic regulation[3][5]. 5-HT2A is the main target of classic hallucinogens such as LSD, psilocin, and DMT, as well as a major site of action for many antipsychotic medications. 5-HT2C is pharmacologically distinct and is notably targeted by lorcaserin for obesity. Both receptors are subjects of intensive clinical and pharmacological research and are considered important therapeutic targets in neuroscience and psychiatry[1][2][3][5].

Other names

Serotonin receptor 2A5-hydroxytryptamine receptor 2AHTR2ASerotonin receptor 2C5-hydroxytryptamine receptor 2CHTR2C

Agonism (psychedelics such as LSD, psilocin activate the receptor); Antagonism (antipsychotics such as risperidone, olanzapine, and pimavanserin inhibit the receptor); Inverse agonism (some drugs stabilize inactive receptor state); Partial agonism (some ligands produce sub-maximal activation); Allosteric modulation (noted for potential but less frequent for this pair)