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Clonidine. Clonidine, sold under the brand name Catapres among others, is an α 2A -adrenergic agonist [12] medication used to treat high blood pressure, ADHD, drug withdrawal (alcohol, opioids, or nicotine), menopausal flushing, diarrhea, spasticity, and certain pain conditions. [13]
Alpha-adrenergic agonist. 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 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]
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.
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.
Tizanidine. Tizanidine, sold under the brand name Zanaflex among others, is an alpha-2 (α 2) adrenergic receptor agonist, [2] similar to clonidine, that is used to treat muscle spasticity due to spinal cord injury, multiple sclerosis, and spastic cerebral palsy. [3] Effectiveness appears similar to baclofen or diazepam. [4]
Centrally acting alpha 2 agonists such as clonidine and guanfacine are thought to most directly target the etiology of NMDA neurotoxicity. Other drugs acting on various neurotransmitter systems known to inhibit NMDA antagonist neurotoxicity include: anticholinergics , diazepam , barbiturates , [ 24 ] ethanol , [ 25 ] 5-HT 2A serotonin receptor ...
Phenoxybenzamine is used as an anti-hypertensive due to its efficacy in reducing the vasoconstriction caused by epinephrine (adrenaline) and norepinephrine. Phenoxybenzamine forms a permanent covalent bond with adrenergic receptors. Based on known information about the structures of these receptors, it likely involves attack by the cysteine at ...