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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 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.
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 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.
So the number of 5-HT 2A receptors decreases through a process known as downregulation and the animal goes back to its normal behavior. This suggests that there are two ways to relieve anxiety in humans with serotonergic drugs: by blocking stimulation of 5-HT 2A receptors or by overstimulating them until they decrease via tolerance.
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.
Most agonists at this receptor are either substituted phenethylamine derivatives from the 2C, DOx and 25-NB groups, or substituted tryptamines and related compounds along with more complex derivatives of these such as lysergamides and iboga-type alkaloids. [1]
In genetics, rs6311 is a gene variation—a single nucleotide polymorphism (SNP)—in the human HTR2A gene that codes for the 5-HT 2A receptor. 5-HT 2A is a neuroreceptor, and several scientific studies have investigated the effect of the genetic variation on personality, e.g., personality traits measured with the Temperament and Character ...