规格: | 98% |
分子量: | 350.39 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
Background:
Potent 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.
Lu et al (2014) PQ-69, a novel and selective adenosine A1 receptor antagonist with inverse agonist activity. Purinergic Signal. 10 619 PMID:25248972