Potent and selective A1
receptor antagonist/inverse agonist. Exhibits high binding affinity at A1
values are 0.07 and 0.96 nM for rat and human receptors respectively). Reduces basal [35
S binding 44.6% (IC50
= 0.19 nM). Antagonizes the effects of A1
agonist R-PIA (IC50
= 18.3 nM) and exhibits competitive antagonism on CCPA
-induced tracheal contractions ex vivo
. Displays 217- fold selectively over hA2A
receptor and >1000-fold selectivity over hA3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity.
Lu et al.
Purinergic Signal., 2014;10:619