Chemical Name: 4-(Butylamino)-2-(3-fluorophenyl)-1,2-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one
Biological ActivityPotent and selective A1 receptor inverse agonist. Exhibits high binding affinity at A1 receptor (Ki values are 0.07 and 0.96 nM for rat and human receptors respectively). Reduces basal [35S]-GTPγS 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 receptor.
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
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