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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 ...
The N-methyl-D-aspartate receptor (NMDA receptor) – a type of ionotropic glutamate receptor – is a ligand-gated ion channel that is gated by the simultaneous binding of glutamate and a co-agonist (i.e., either D-serine or glycine). [11] Studies show that the NMDA receptor is involved in regulating synaptic plasticity and memory. [12] [13]
5-HT 1A receptor (as partial or full agonists) 5-HT 2A receptor (as inverse agonists) D 2 receptor (as antagonists or partial agonists) α 1-adrenergic receptor (as antagonists) α 2-adrenergic receptor (as antagonists) Actions at D 4, 5-HT 2C, 5-HT 7, and sigma receptors have also been shown for some azapirones. [33] [34] [35] [36]
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.
In contrast to α 2-adrenergic receptors, α 1-adrenergic-receptors in the arterial vasculature of skeletal muscle are more resistant to inhibition, and attenuation of α1-adrenergic-receptor-mediated vasoconstriction only occurs during heavy exercise. [18] Note that only active muscle α 1-adrenergic receptors will
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 norepinephrine being the highest affinity.
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]
An atypical example is given by the β-adrenergic autoreceptor in the sympathetic peripheral nervous system, which acts to increase transmitter release. [1] The D2 autoreceptor has been shown recently to interact with the trace amine-associated receptor 1 (TAAR1), a G-Coupled Protein Receptor GPCR, to regulate monoaminergic systems in the brain ...