DPTN is a potent and selective human, mouse, and rat A3AR antagonist with Ki values of 1.65, 9.61, and 8.53nM, respectively.
DPTN is indeed a potent antagonist for human, mouse, and rat A3ARs . DPTN is weaker at mouse and rat compared with human A3AR and has reduced selectivity (about 20-fold vs A2BAR).[1].
The Binding affinity of BNPT (10 μM) is tested in membranes of transfected HEK293 cells, the Ki values are 162 ± 49, 121 ± 42, 230 ± 40, and 1.65 ± 0.57 nM for hA1, hA2A, hA2B, and hA3, respectively[1].
DPTN’s Ki values at respective A1, A2A, A2B, and A3 receptors are 411, 830, 189, and 9.61 nM (mouse); and 333, 1147, 163, and 8.53 nM (rat) [1].
References:
[1]. Zhan-Guo Gao, et al. Pharmacological characterization of DPTN and other selective A3 adenosine receptor antagonist. Purinergic Signal. 2021 Dec;17(4):737-746.