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Furthermore, located in the intracellular side close to the membrane is a small alpha helix, often referred to as helix 8 (H8). The crystallographic structure of the adenosine A 2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). [7]
Caffeine keeps you awake by blocking adenosine receptors. Each type of adenosine receptor has different functions, although with some overlap. [3] For instance, both A 1 receptors and A 2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A 2A receptor also has broader anti-inflammatory effects throughout the body. [4]
A 2A receptors are G-protein coupled receptor (GPCR) that increases cyclic adenosine monophosphate (cAMP). [7] [1] These receptors are mainly expressed in the brain. [11] After almost a century of receptor research, the adenosine A 2A receptor has been selected as a possible research target for various medical conditions. [1]
Two subtypes of adenosine A 2 receptors are known. Both are G protein-coupled adenosine receptors: Adenosine A 2A receptor; Adenosine A 2B receptor
The affinities (K i) of MSX-2 for the human adenosine receptors are 5.38 to 14.5 nM for the adenosine A 2A receptor, 2,500 nM for the adenosine A 1 receptor (172- to 465-fold lower than for the A 2A receptor), and >10,000 nM for the adenosine A 2B and A 3 receptors (>690-fold lower than for the A 2A receptor). [3] [4]
These receptors enable the regulation of multiple processes such as cell proliferation, differentiation, function, and death. [47] The activation of the adenosine A1 receptor is required for osteoclast differentiation and function, whereas the activation of the adenosine A2A receptor inhibits osteoclast function. The other three adenosine ...
Such heteromers may be between receptors from the same family (e.g., adenosine A 1 /A 2A heteromers [9] [10] and dopamine D 1 /D 2 [11] and D 1 /D 3 heteromers [12]) or between entirely unrelated receptors such as CB 1 /A 2A, [13] glutamate mGluR 5 / adenosine A 2A heteromers, [14] cannabinoid CB 1 / dopamine D 2 heteromers, [15] and even CB 1 ...
ZM-241,385 is a high affinity antagonist ligand selective for the adenosine A 2A receptor. [1]In animal models, ZM-241,385 has been shown to protect against beta amyloid neurotoxicity and therefore may be useful as a treatment for Alzheimer's disease. [2]