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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.
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 .
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.
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.
In genetics, rs6314, also called His452Tyr or H452Y, is a gene variation, a single nucleotide polymorphism (SNP), in the HTR2A gene that codes for the 5-HT 2A receptor.The SNP is located in exon 3 of the gene and the change between C and T results in a change between histidine (His) and tyrosine (Tyr) at the 452nd amino acid, i.e., it is a missense substitution.
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.
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 HTR is a rapid, rhythmic side-to-side or rotational head movement that intermittently occurs in mice and rats in association with serotonin 5-HT 2A receptor activation. [1] [2] In mice, each individual head movement lasts about 10 milliseconds and each HTR consists of 5 to 11 individual head movements.