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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-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
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]
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]
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] It is taken by mouth. [5]
Alpha-2 adrenergic agonists such as clonidine are traditionally used to treat hypertension via inhibition of norepinephrine release. [17] Central alpha-2 adrenergic activation in the locus ceruleus and spinal cord induce sedation and pain modulation respectively. [17] Clonidine has been shown to have some efficacy when treating both acute and ...
Increased level of norepinephrine increases the basal activity of alpha-2 adrenergic receptors, which mediate an analgesic effect by increasing gamma-aminobutyric acid transmission among spinal interneurons. The blocking effect of amitriptyline on sodium channels may also contribute to its efficacy in pain conditions. [6]
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.