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The 5-HT 1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation. 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems.
Azapirones such as buspirone, gepirone, and tandospirone are 5-HT 1A receptor partial agonists marketed primarily as anxiolytics, but also as antidepressants. The antidepressants vilazodone and vortioxetine are 5-HT 1A receptor partial agonists. Flibanserin, a drug used for female sexual dysfunction, is a 5-HT 1A receptor partial agonist.
5-HT receptors were split into two classes by John Gaddum and Picarelli when it was discovered that some of the serotonin-induced changes in the gut could be blocked by morphine, while the remainder of the response was inhibited by dibenzyline, leading to the naming of M and D receptors, respectively. 5-HT 2A is thought to correspond to what was originally described as D subtype of 5-HT ...
A 5-HT 2C agonist may be expected to reduce positive symptoms of schizophrenia by reducing dopamine release in the mesolimbic dopamine pathway. Vabicaserin (SCA-136) is a 5-HT 2C agonist that has shown promise in preliminary testing for the treatment of schizophrenia. [42]
The 5-HT 1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT 1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus.
Several drugs that act as 5-HT 4 selective agonists have recently been introduced into use in both scientific research and clinical medicine. Some drugs that act as 5-HT 4 agonists are also active as 5-HT 3 antagonists, such as mosapride, metoclopramide, renzapride, and zacopride, and so these compounds cannot be considered highly selective.
5-Hydroxytryptamine (serotonin) receptor 5A, also known as HTR5A, is a protein that in humans is encoded by the HTR5A gene. [5] [6] Agonists and antagonists for 5-HT receptors, as well as serotonin uptake inhibitors, present promnesic (memory-promoting) and/or anti-amnesic effects under different conditions, and 5-HT receptors are also associated with neural changes.
This is a list of miscellaneous agonists of the serotonin receptor subtype 5-HT 2A (and other 5-HT 2 subtypes to a varying extent) that fall outside the common structural classes.