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The alpha-2 (α 2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the G i heterotrimeric G-protein. It consists of three highly homologous subtypes, including α 2A-, α 2B-, and α 2C-adrenergic. Some species other than humans express a fourth α 2D-adrenergic receptor as well. [1]
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β 2) antagonists and alpha-2 (α 2) agonists, which are used to treat high ...
Agonists of alpha-2 receptors in the vascular smooth muscle lead to vasoconstriction. However, in clinical practice drugs applied intravenously that are agonists of alpha-2 receptors such as clonidine lead to powerful vasodilation, which causes a decrease in blood pressure by presynaptic activation of the receptors in the sympathetic ganglia.
The alpha-2 blocker acts on alpha-2 receptors. The alpha-2 receptor is a G-protein coupled receptor as well, which exert its action by Gi function, leading to an inhibition of adenylyl cyclase and thus reducing synthesis of cAMP. [3] It lowers the amount of calcium inside the cell. [3]
The alpha-adrenergic receptor has two subclasses α 1 and α 2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with
Major autoreceptor which clinically important are alpha 2(adrenergic receptor subtype 2), H 3(histamine receptor subtype 3), 5 HT 1(serotonin receptor subtype 1). In which respective drugs act are Clonidine on alpha 2 as Agonist used in hypertension which reduce release of norepinephrine and epinephrine from presynaptic neurons.
150 11551 Ensembl ENSG00000150594 ENSMUSG00000033717 UniProt P08913 Q01338 RefSeq (mRNA) NM_000681 NM_007417 RefSeq (protein) NP_000672 NP_031443 Location (UCSC) Chr 10: 111.08 – 111.08 Mb Chr 19: 54.03 – 54.04 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse The alpha-2A adrenergic receptor (α 2A adrenoceptor), also known as ADRA2A, is an α 2 -adrenergic receptor, and also ...
They act by antagonizing the α 2-adrenergic receptor and certain serotonin receptors such as 5-HT 2A and 5-HT 2C, [1] but also 5-HT 3, [1] 5-HT 6, and/or 5-HT 7 in some cases. By blocking α 2 -adrenergic autoreceptors and heteroreceptors , NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation ...