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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 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.
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.
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.
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.
25N-NBPh (NBPh-2C-N) is a phenethylamine derivative from the 25-NB class, which acts as a potent agonist at the 5-HT 2A receptor with weaker activity at 5-HT 2B and 5-HT 2C. 25N-NBPh is a biased agonist, producing robust activation of 5-HT 2A coupled signalling pathways mediated by beta arrestin 2, but with only slight activation of pathways mediated via G q.
An alternative for PET imaging the 5-HT 2A receptor is the [11 C]volinanserin (MDL-100,907) radioligand. 18 F-altanserin and 3 H-volinanserin have shown very comparable binding. [3] Both altanserin and MDL 100,907 are 5-HT 2A receptor antagonists. [3] [18 F]-setoperone can also be used in PET.