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In Wikidata. Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. 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.
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) agonists and alpha-2 (α 2) agonists, which are used to treat high blood ...
Adrenergic agonist. An adrenergic agonist is a drug that stimulates a response from the adrenergic receptors. The five main categories of adrenergic receptors are: α 1, α 2, β 1, β 2, and β 3, although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively.
Alpha-1 adrenergic receptor. alpha-1 (α1) adrenergic receptors are G protein-coupled receptors (GPCRs) associated with the G q heterotrimeric G protein. α 1 -adrenergic receptors are subdivided into three highly homologous subtypes, i.e., α 1A -, α 1B -, and α 1D -adrenergic receptor subtypes. There is no α 1C receptor.
The alpha-2 (α2) 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]
As of 2018, prazosin is the only alpha-1 blocker known to act as an inverse agonist at all alpha-1 adrenergic receptor subtypes; [3] [4] whereas tamsulosin is a selective antagonist for all alpha-1 subtypes. [3] [5] Drugs that act as selective antagonists at specific alpha-1 adrenergic receptor subtypes have also been developed.
A primary or secondary aliphatic amine separated by 2 carbons from a substituted benzene ring is minimally required for high agonist activity. The pKa of the amine is approximately 8.5-10. [2] The presence of hydroxy group in the benzene ring at 3rd and 4th position shows maximum alpha- and beta-adrenergic activity. [medical citation needed]
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.
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