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A pyrazolo[4,3- e ][1,2,4]triazolo[1,5- c ]pyrimidin-5-amine antagonist of the A 2A adenosine receptor (AR) was functionalized as amine congeners, fluorescent conjugates and a sulfonate, and the A 2A AR binding modes were predicted computationally. The optimal n -butyl spacer was incorporated into the following A 2A AR-selective ( K  i , nM) conjugates: BODIPY630/650 derivative 11 (MRS7396, 24.6) and AlexaFluor488 derivative 12 (MRS7416, 30.3). Flow cytometry of 12 in hA 2A AR-expressing HEK-293 cells displayed saturable binding (low nonspecific) and inhibition by known A 2A AR antagonists. Water-soluble sulfonate 13 was a highly potent ( K  i = 6.2 nM) and selective A 2A AR antagonist based on binding and functional assays. Docking and molecular dynamics simulations predicted the regions of interaction of the distal portions of these chain-extended ligands with the A 2A AR. The BODIPY630/650 fluorophore of 11 was buried in a hydrophobic interhelical (TM1/TM7) region, while AlexaFluor488 of 12 associated with the hydrophilic extracellular loops. In conclusion, we have identified novel high affinity antagonist probes for A 2A AR drug discovery and characterization.

medchemcomm

Bitopic fluorescent antagonists of the A<sub>2A</sub> adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners

Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners

Bitopic fluorescent antagonists of the A_2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners