Chemical Name: 4-(Butylamino)-2-(3-fluorophenyl)-1,2-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one
Biological Activity Potent and selective A1 receptor antagonist/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.
Soluble to 100 mM in DMSO and to 10 mM in ethanol with gentle warming
Store at +4°C
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