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:
“Our father has an even more important function than modeling manhood for us. He is also the authority to let us relax the requirements of the masculine model: if our father accepts us, then that declares us masculine enough to join the company of men. We, in effect, have our diploma in masculinity and can go on to develop other skills.”
—Frank Pittman (20th century)
“Morality and its victim, the mother—what a terrible picture! Is there indeed anything more terrible, more criminal, than our glorified sacred function of motherhood?”
—Emma Goldman (1869–1940)
“The mother’s and father’s attitudes toward the child correspond to the child’s own needs.... Mother has the function of making him secure in life, father has the function of teaching him, guiding him to cope with those problems with which the particular society the child has been born into confronts him.”
—Erich Fromm (1900–1980)