5-hydroxytryptamine receptor 2A, 2B, 2C, 3, 6, and 7 (5-HT2A/2B/2C/3/6/7)

The 5-HT2A/2B/2C/3/6/7 receptors represent a diverse subset of the serotonin (5-hydroxytryptamine) receptor family, encompassing both G protein-coupled receptors (5-HT2A, 2B, 2C, 6, and 7) and a ligand-gated ion channel (5-HT3) [1, 3, 4]. These receptors are widely distributed throughout the central and peripheral nervous systems, where they modulate critical physiological processes including mood, cognition, perception, appetite, and gastrointestinal motility [3, 5, 13]. Specifically, the 5-HT2 subfamily is primarily involved in psychiatric regulation and smooth muscle function, while 5-HT3 mediates rapid excitatory neurotransmission and emetic responses [1, 10, 14]. The 5-HT6 and 5-HT7 receptors are key players in cognitive processing and circadian rhythms [13]. This multi-receptor profile is a primary therapeutic target for atypical antipsychotics and multi-modal antidepressants, which often act as antagonists or inverse agonists to treat schizophrenia, bipolar disorder, and major depressive disorder [1, 6, 9]. However, off-target activation, particularly of the 5-HT2B receptor, is associated with serious safety concerns such as cardiac valvulopathy, while 5-HT2C modulation is linked to metabolic side effects [11, 18, 19].

Other names

Serotonin receptors 2A/2B/2C/3/6/75-HT2/3/6/7 receptorsHTR2A/HTR2B/HTR2C/HTR3/HTR6/HTR75-hydroxytryptamine receptor subtypes

Antagonism, inverse agonism, and agonism of various serotonin receptor subtypes to modulate neurotransmitter release (e.g., dopamine, glutamate) and intracellular signaling pathways such as Gq/PLC (5-HT2) and Gs/adenylyl cyclase (5-HT6/7) [4, 7, 10, 13].