5-HT is involved in a diverse array of physiological and biological processes. In the brain, 5-HT affects sleep, mood, appetite, anxiety, aggression, perception, pain, and cognition¹. Signaling of 5-HT is mediated by receptors that are located on the cell membrane of neurons and most other cells in the body. The 5-HT2 family consists of three G-protein coupled receptors (GPCRs): 5-HT2A, 5-HT2B, and 5-HT2C². They are transmembrane proteins consisting of seven membrane-spanning α-helical segments with an extracellular N-terminus and an intracellular C-terminus. The binding of 5-HT to one of its receptors is thought to elicit a conformational change that activates associated heterotrimeric G proteins and recruits other downstream signaling/scaffolding molecules, such as GPCR kinases and β-arrestins.

5-HT2A receptors have been found in many regions of the human brain including the cortex, brainstem, olfactory bulb, limbic system and basal ganglia³.

The 5-HT2A receptor has been implicated in many mental disorders including schizophrenia, depression, obsessive compulsive disorder (OCD), attention deficit–hyperactivity disorder (ADHD), and eating disorders such as anorexia nervosa and autism spectrum disorders⁴.