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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.
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]
Pituitary gland tumors are very common in the canine. A productive form arising from the anterior pituitary is the primary cause of Cushing's disease of dogs. This tumor causes excessive production of cortisol from the adrenal cortex which leads to the classic signs of alopecia (hair loss), polyuria (excessive urination), polydipsia (excessive water drinking), and a pot-bellied appearance of ...
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]
It acts as an antagonist at the 5-HT 2A receptor, [2] as an inverse agonist at the 5-HT 2C receptor, [3] and as a GABA reuptake inhibitor. [4] The two serotonin receptors are G protein-coupled receptors and are two of the main excitatory serotonin receptor types. Their excitation has been implicated in anxiety and mood. [5]
The development of 5-HT 2C agonists has been a major obstacle, because of severe side effects due to a lack of selectivity over 5-HT 2A and 5-HT 2B receptors. Activation of 5-HT 2A receptors can induce hallucinations, and the activation of 5-HT 2B receptors has been implicated in cardiac valvular insufficiency and possibly in pulmonary ...
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 .
SB-221284 is a selective serotonin 5-HT 2C and 5-HT 2B receptor antagonist which is used in scientific research. [1] [2] [3]Its affinities (K i) are 2.2 to 2.5 nM for the serotonin 5-HT 2C receptor, 2.5 to 12.6 nM for the serotonin 5-HT 2B receptor, and 398 to 550 nM for the serotonin 5-HT 2A receptor (where it is also an antagonist).
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