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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 ...
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]
They are mainly used in research, having found limited clinical application in human medicine. They are extensively used in veterinary medicine to reverse the effects of alpha-2 agonist drugs used as sedatives, like xylazine, medetomidine and dexmedetomidine. Alpha-2 blockers increase noradrenaline release.
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.
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]