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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.
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.
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]
Dexmedetomidine is a highly selective α 2-adrenergic receptor agonist. It possesses an α 2:α 1 selectivity ratio of 1620:1, making it 8 times more selective for the α 2-adrenergic receptor than the related drug clonidine.
Apart from increasing the noradrenaline release, the selective alpha-2 blockers have the potential to bind with other receptors such as the 5-HT serotonin receptor. [10] However, the serotonin receptor antagonism has side effects such as weight gain and impaired movement. [11] Hence, alpha-2 blockers are not used clinically due to its extensive ...
Medetomidine is a racemic mixture of two optical or stereoisomers, levomedetomidine and dexmedetomidine. [4] The latter causes the alpha 2- adrenergic agonist effects. [5] It is often used as the hydrochloride salt, medetomidine hydrochloride, a crystalline white solid that can be administered as an intravenous drug solution with sterile water.
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 ...
Xylazine is a potent α 2-adrenergic receptor agonist. [23] [3] When xylazine and other α 2-adrenergic receptor agonists are administered, they distribute throughout the body within 30 to 40 minutes. [17]