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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]
Gabapentinoid. Gabapentinoids, also known as α2δ ligands, are a class of drugs that are derivatives of the inhibitory neurotransmitter gamma-Aminobutyric acid (GABA) (i.e., GABA analogues) which block α 2 δ subunit -containing voltage-dependent calcium channels (VDCCs). [1][2][3][4] This site has been referred to as the gabapentin receptor ...
Gabapentin is a ligand of the α 2 δ calcium channel subunit. [82] [83] α 2 δ is an auxiliary protein connected to the main α 1 subunit (the channel-forming protein) of high voltage activated voltage-dependent calcium channels (L-type, N-type, P/Q type, and R-type). [13]
Guanfacine, sold under the brand name Tenex (immediate-release) and Intuniv (extended-release) among others, is an oral alpha-2a agonist medication used to treat attention deficit hyperactivity disorder (ADHD) and high blood pressure. [3][9] Guanfacine is FDA-approved for monotherapy treatment of ADHD, [3] as well as being used for augmentation ...
Methyldopa acts on alpha-2 adrenergic receptors, which are found on the pre synaptic nerve terminal. [1] This inhibits the synthesis of norepinephrine by inhibiting tyrosine hydroxylase . The S-enantiomer of methyldopa is a competitive inhibitor of the enzyme aromatic L -amino acid decarboxylase (LAAD), which converts L -DOPA into dopamine .
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Beta-1 adrenergic receptor. The beta-1 adrenergic receptor (β 1 adrenoceptor), also known as ADRB1, can refer to either the protein-encoding gene (gene ADRB1) or one of the four adrenergic receptors. [5] It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein that is expressed predominantly in cardiac tissue.
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