[5][8][9] Based on its abundance in extrapyramidal, limbic, and cortical regions it can be suggested that the 5HT6 receptor plays a role in functions like motor control, emotionality, cognition, and memory.

[7][9][10] Blockade of central 5HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas,[11][12][13][14] whereas activation enhances GABAergic signaling in a widespread manner.

[15] Antagonism of 5HT6 receptors also facilitates dopamine and norepinephrine release in the frontal cortex,[14][16] while stimulation has the opposite effect.

[15] Despite the 5HT6 receptor having a functionally excitatory action, it is largely co-localized with GABAergic neurons and therefore produces an overall inhibition of brain activity.

[20][21] Recently, the 5HT6 agonists WAY-181,187 and WAY-208,466 have been demonstrated to be active in rodent models of depression, anxiety, and obsessive-compulsive disorder (OCD), and such agents may be useful treatments for these conditions.