Adenosine A2AR fluorescent probe
Tag-lite Adenosine A2A receptor fluorescent probe
One of four adenosine receptors found in the brain, A2A is a GPCR. A2A receptor is thought to play a role in acute and chronic neurodegenerative disorders such as cerebral ischemia or Parkinson's disease. A2A may also be involved in seizures and sleep disorders.
Cells expressing the A2A receptor are provided pre-labeled with Terbium, and can be used to conduct receptor binding studies on the aforementioned receptor.
Examples of data obtained using A2A labeled cells and their matching fluorescent ligand (L0058RED). ZM-241385 was used as reference ligand. Results may vary from one HTRF® compatible reader to another.
Adenosine receptors designated by four subtypes A1, A2A, A2B and A3 were shown to be promising pharmacological targets for the development of therapeutic compounds for various therapeutic areas such as cancer, neurodegenerative disease and COPD/Asthma. Thus, a wide range of compounds, and particularly antagonists have been largely studied.
The Tag-Lite® binding assay platform offers the complete adenosine receptors subset A1, A2A, A2B and A3 to characterize compounds in term of binding affinity (Ki) and selectivity profile.
The set of compounds have been profiled on A1, A2A, A2B and A3 receptors using their respective fluorescent ligands L0067RED, L0058RED, L0068RED and L0069GRE.The selectivity profiles of several compounds involved in different therapeutic areas were assessed with this Tag-Lite platform.
The table below summarizes the resulting Ki obtained for each receptor subtype for the full panel of compounds. The results are confirming the expected selectivity and the range of affinities for these reference compounds.
|Compound||Pharmacological class||Compounds affinities (Ki - nM) for the different adenosine receptor subtypes|
|XAC||Non selective antagonist||12||15||20||50|
|Theophylline||Non selective antagonist||4000||5000||18000||140000|
|Ciforadenant (CPI-444)||A2A antagonist||150||3.4||660||1600|
|Preladenant (SCH 420814)||A2A antagonist||> 20 000||5||> 20 000||>20 000|
|Istradefylline (KW-6002)||A2A antagonist||>10 000||40||>10 000||>10 000|
|AZD4635||A2A antagonist||900||15||660||> 10 000|
|MRS1706||A2B inverse agonist||150||325||30||> 300|
|MRS1220||A3 antagonist||325||37||> 500||1.6|
The graphs show the pattern of the dose-response curves obtained for five compounds displaying different selectivity profile.
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