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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
In non-human species this is an immobilizing and anesthetic drug, presumptively also mediated by α 2 adrenergic receptors because it is reversed by yohimbine, an α 2 antagonist. α 2A selective agonists include guanfacine (an antihypertensive) and brimonidine (UK 14,304). -3-nitrobiphenyline is an α 2C selective agonist as well as being a ...
The tetracyclic antidepressants mianserin and mirtazapine are α 2 blockers, although their efficacy as antidepressants may come from their activity at other receptor sites. [citation needed] Mechanistically, α 2 blockers increase adrenergic, dopaminergic and serotonergic neurotransmitters and induce insulin secretion, decreasing blood sugar ...
US: ℞-only [2] Medetomidine/vatinoxan , sold under the brand name Zenalpha , is a veterinary fixed dose combination medication used as a sedative and analgesic for dogs. [ 1 ] [ 2 ] It contains medetomidine , an alpha2-adrenoceptor agonist, as the hydrochloride; and vatinoxan , an alpha2-adrenoceptor antagonist, as the hydrochloride.
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.
Drugs that meet these needs are opioids, benzodiazepines, alpha-2 agonists, neurosteroids, and dissociatives. Alpha-2 agonists can be used alone in dogs and cats to produce this effect. A combination of Alpha-2 agonists and neurosteroids or dissociatives also achieve the same effect. [3]
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]
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]