PQ 69

Biological Activity

PQ 69 is a potent and selective A₁ receptor inverse agonist. Exhibits high binding affinity at A₁ receptor (K_i 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 hA_2A receptor and >1000-fold selectivity over hA₃ receptor.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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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