General Description
A cell-permeable adenosine analog that acts a potent non-selective agonist of adenosine receptors (K
i = 14 nM, 20 nM, 2.4 μM and 6.2 nM for A
1, A
2A, A
2B, A
3, respectively). Increases intracellular cAMP production (EC
50 = 3.1 μM in A
2B expressing CHO cells). Shown to increase glucagon release in a dose-dependent manner and inhibit insulin release at low concentrations. Although at higher concentration some insulin release is observed. Also, displays a wide range adenosine-dependent effects, such as blocking platelet aggregation and inhibiting DNA synthesis. When administered at reperfusion, it is shown reduce infarction and block the formation of the mitochondrial permeability transition pore by activating p70S6 kinase.
Biological Activity
Potent adenosine receptor agonist (K i values are 14, 20 and 6.2 nM for human A 1 , A 2A and A 3 receptors respectively; EC 50 = 2.4 μ M for human A 2B ). Inhibits platelet aggregation and is centrally active in vivo .
