Function
Blockade of central 5-HT6 receptors has been shown to increase glutamatergic and cholinergic neurotransmission in various brain areas, whereas activation enhances GABAergic signaling in a widespread manner. Antagonism of 5-HT6 receptors also facilitates dopamine and norepinephrine release in the frontal cortex, while stimulation has the opposite effect.
Despite the 5-HT6 receptor having a functionally excitatory action, it is largely co-localized with GABAergic neurons and therefore produces an overall inhibition of brain activity. In parallel with this, 5-HT6 antagonists improve cognition, learning, and memory, and agents such as latrepirdine, Lu AE58054, and SB-742,457 are being developed as novel treatments for Alzheimer's disease and other forms of dementia. 5-HT6 antagonists have also been shown to reduce appetite and produce weight loss, and as a result, PRX-07034, BVT-5,182, and BVT-74,316 are being investigated for the treatment of obesity.
Recently, the 5-HT6 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. Additionally, it can be inferred that 5-HT6 activation likely plays a major role in the therapeutic benefits of serotonergic antidepressants like the selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants (TCAs).
Read more about this topic: 5-HT6 Receptor
Famous quotes containing the word function:
“The function of muscle is to pull and not to push, except in the case of the genitals and the tongue.”
—Leonardo Da Vinci (1425–1519)
“We are thus able to distinguish thinking as the function which is to a large extent linguistic.”
—Benjamin Lee Whorf (1897–1934)
“Philosophical questions are not by their nature insoluble. They are, indeed, radically different from scientific questions, because they concern the implications and other interrelations of ideas, not the order of physical events; their answers are interpretations instead of factual reports, and their function is to increase not our knowledge of nature, but our understanding of what we know.”
—Susanne K. Langer (1895–1985)