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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 ...
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.
Selective 5-HT2A receptor agonists (10 P) Pages in category "5-HT2A agonists" The following 43 pages are in this category, out of 43 total.
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.
GM-2040 is a putatively non-hallucinogenic serotonin 5-HT 2A receptor agonist which was developed by Gilgamesh Pharmaceuticals. [1] It is a partial agonist of the serotonin 5-HT 2A receptor, with a K i of 3.4 nM, an EC 50 Tooltip half-maximal effective concentration of 43.8 nM, and an E max Tooltip maximal efficacy of 71.1%. [1]
Non-hallucinogenic serotonin 5-HT 2A receptor agonists, either due to being biased agonists, partial agonists, or peripherally selective. Some of these agents may be weakly hallucinogenic or hallucinogenic only at very high doses rather than fully non-hallucinogenic.
ITI-1549 is a putatively non-hallucinogenic serotonin 5-HT 2A receptor agonist which is under development for the treatment of mood disorders and other psychiatric disorders. [1] [4] [5] [2] [3] In addition to acting at the serotonin 5-HT 2A receptor, it is also an antagonist of the serotonin 5-HT 2B receptor and an agonist of the serotonin 5-HT 2C receptor.
The development of 5-HT 2C agonists has been a major obstacle, because of severe side effects due to a lack of selectivity over 5-HT 2A and 5-HT 2B receptors. Activation of 5-HT 2A receptors can induce hallucinations, and the activation of 5-HT 2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary ...