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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]
The alpha-2 (α2) 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]
Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. [1] [2] [3] There are three main classes of imidazoline receptor: I 1 is involved in inhibition of the sympathetic nervous system to lower blood pressure, [4] I 2 has as yet uncertain functions but is implicated in several psychiatric conditions, [5] [6] and I 3 regulates insulin secretion.
Clonidine, an alpha-2 receptor agonist, is another drug that has found use as an analgesic adjuvant. [81] In 2021, researchers described a novel type of pain therapy — a CRISPR-dCas9 epigenome editing method for repressing Na v 1.7 gene expression which showed therapeutic potential in three mouse models of chronic pain. [83] [84]
A sympatholytic (sympathoplegic) drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). [1] They are indicated for various functions; for example, they may be used as antihypertensives. They are also used to treat anxiety, such as generalized ...
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.
Alpha-2 blockers (or α2 blockers) are a subset of the alpha blocker class of drugs and are antagonists to the α 2 adrenergic receptor. 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 ...
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.