Adenosine A1 Receptor Antagonist I

A blood-brain barrier permeable xanthine derivative that acts as a highly selective antagonist of Adenosine A1 receptor (A1R; Ki = 3.9 nM, 130 nM, 1.0 µM, 4.0 µM for human A1, A2A, A2B, and A3 respectively). Exhibits about 1,000-fold higher affinity and a 30-fold greater selectivity for A1R when compared to theophylline. Shown to competitively antagonize the inhibition of adenylate cyclase activity via A1 adenosine receptors in rat fat cells and the stimulation of adenylate cyclase via A2 adenosine receptors in human platelets. Exhibits hypertensive properties.