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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]
Major autoreceptor which clinically important are alpha 2(adrenergic receptor subtype 2), H 3(histamine receptor subtype 3), 5 HT 1(serotonin receptor subtype 1). In which respective drugs act are Clonidine on alpha 2 as Agonist used in hypertension which reduce release of norepinephrine and epinephrine from presynaptic neurons.
150 11551 Ensembl ENSG00000150594 ENSMUSG00000033717 UniProt P08913 Q01338 RefSeq (mRNA) NM_000681 NM_007417 RefSeq (protein) NP_000672 NP_031443 Location (UCSC) Chr 10: 111.08 – 111.08 Mb Chr 19: 54.03 – 54.04 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse The alpha-2A adrenergic receptor (α 2A adrenoceptor), also known as ADRA2A, is an α 2 adrenergic receptor, and also ...
It is a presynaptic receptor, causing negative feedback on, for example, norepinephrine (NE). When NE is released into the synapse, it feeds back on the α 2 receptor, causing less NE release from the presynaptic neuron. This decreases the effect of NE. There are also α 2 receptors on the nerve terminal membrane of the post-synaptic adrenergic ...
Additionally, the receptors on the post-synaptic side also play a role, both in their numbers, composition, and physical orientation. Some of these mechanisms rely on changes in both the presynaptic and postsynaptic neurons, resulting in a prolonged modification of the synaptic potential. [7]
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]
Postsynaptic potentials occur when the presynaptic neuron releases neurotransmitters into the synaptic cleft. These neurotransmitters bind to receptors on the postsynaptic terminal, which may be a neuron , or a muscle cell in the case of a neuromuscular junction . [ 1 ]
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.