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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 exception to this is the 5-HT 3 receptor which is a ligand-gated ion channel. In 2014, a novel 5-HT receptor was isolated from the small white butterfly, Pieris rapae, and named pr5-HT 8. It does not occur in mammals and shares relatively low similarity to the known 5-HT receptor classes. [7]
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 .
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.
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.
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]
The VTA contains 5-HT 1A receptors that exert a biphasic effects on firing, with low doses of 5-HT 1A receptor agonists eliciting an increase in firing rate, and higher doses suppressing activity. The 5-HT 2A receptors expressed on dopaminergic neurons increase activity, while 5-HT 2C receptors elicit a decrease in activity. [39]
In mammals, substantial concentrations of 5-HT are present in the central and peripheral nervous systems, gastrointestinal tract and cardiovascular system. 5-HT is capable of exerting a wide variety of biological effects by interacting with specific membrane-bound receptors, and at least 13 distinct 5-HT receptor subtypes have been cloned and ...