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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.
alpha-1 (α 1) 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.
Currently, several relatively selective alpha-1 antagonists are available. 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 and terazosin are both selective antagonists for all alpha-1 subtypes.
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.
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.
Alpha blockers, also known as α-blockers or α-adrenoreceptor antagonists, are a class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). [ 2 ] Historically, alpha-blockers were used as a tool for pharmacologic research to develop a greater understanding of the autonomic nervous system.
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.
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 ...