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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-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.
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.
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.
Intuniv - an extended release, non-stimulant alpha-2 adrenergic agonist used to treat attention deficit hyperactivity disorder. Available in instant-release under the brand-name Tenex . Invega ( paliperidone ) – atypical antipsychotic used to treat schizophrenia and schizoaffective disorder
Clonidine, sold under the brand name Catapres among others, is an α 2A-adrenergic receptor agonist [12] medication used to treat high blood pressure, ADHD, drug withdrawal (e.g., alcohol, opioids, or nicotine), menopausal flushing, diarrhea, spasticity, and certain pain conditions. [13]
In addition, there is continuing research and development of new dual α/δ and γ/δ PPAR agonists for additional therapeutic indications, as well as "pan" agonists acting on all three isoforms. [7] [8] The anti-hypertension drug telmisartan is known to have PPAR γ/δ dual partial agonist activity in vivo. It also activates PPAR-α in vitro. [9]
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]