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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 ...
Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants. [1] 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.
Many tricyclic antidepressants, tetracyclic antidepressants, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole antagonize α 1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
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. However, there are also other mechanisms ...
An adrenergic antagonist is a drug that inhibits the function of adrenergic receptors. There are five adrenergic receptors, which are divided into two groups. The first group of receptors are the beta (β) adrenergic receptors. There are β 1, β 2, and β 3 receptors. The second group contains the alpha (α) adrenoreceptors.
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]
Alpha 1 blocker exerts its action on alpha-1 receptor, dilating the smooth muscles. [3] Alpha-1 receptor is a Gq type G-protein coupled receptor. [3] When it is activated, it will lead to activation of phospholipase C, raising the intracellular level of IP3 and DAG. [3]
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.