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The 5-HT 2A receptor is a subtype of the 5-HT 2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). [4] The 5-HT 2A receptor is a cell surface receptor, [5] but has several intracellular locations. [6] Like all 5-HT 2 receptors, the 5-HT 2A receptor is G q /G 11-protein coupled.
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.
The 5-HT 2 receptors are a subfamily of 5-HT receptors that bind the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). [1] The 5-HT 2 subfamily consists of three G protein-coupled receptors (GPCRs) which are coupled to G q /G 11 and mediate excitatory neurotransmission , [ 2 ] including 5-HT 2A , 5-HT 2B , and 5-HT 2C .
An example of upregulation is the response of liver cells exposed to such xenobiotic molecules as dioxin. In this situation, the cells increase their production of cytochrome P450 enzymes, which in turn increases degradation of these dioxin molecules. Downregulation or upregulation of an RNA or protein may also arise by an epigenetic alteration ...
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.
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.
Serotonin (/ ˌ s ɛr ə ˈ t oʊ n ɪ n, ˌ s ɪər ə-/) [6] [7] [8] or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter.Its biological function is complex, touching on diverse functions including mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction.
There are however numerous 5-HT 2A receptor agonists which do not fall within any of these groups, some representative examples of which are listed below. K i and EC 50 values vary depending on the assay conditions used and so may not be directly comparable between sources.