Pharmacological properties of T1-11.

Binding properties of T1-11 toward four adenosine receptors (A1, A2A, A2B, and A3 receptors) and one adenosine transporter (ENT1) were conducted and characterized using standard binding protocols. T1-11 is an agonist of the A2AR to activate adenylyl cyclases and subsequently elevate cellular cAMP levels (Fig. 2). T1-11 also suppressed the uptake of adenosine (Fig. 3), and therefore was considered an inhibitor of ENT1. No significant binding of T1-11 toward the A1R or A2BR at 10 µM was found. Although T1-11 also bound to the A3R, it evoked no significant GTPγS binding at a concentration (10 µM) 1000-fold of its 1000-fold of its Ki value. n.d., not determined. n.s., not significant.