Piclidenoson

Piclidenoson is an adenosine A₃ receptor agonist (K_i = 1.7 nM).¹ It is selective for adenosine A₃ over A₁ and A₂ receptors (K_is = 55.3 and 3,099 nM, respectively). In vivo, piclidenoson (100 µg/kg) reduces wall thickening in a rabbit model of ischemia-reperfusion injury induced by coronary artery occlusion, an effect that can be reversed by the adenosine receptor antagonist 8-p-sulfophenyl theophylline.² It reduces hepatocellular tumor growth, liver inflammation, and neuropathy in a rat model of bone-residing breast cancer and decreases the number of lung metastases in a model of metastatic murine melanoma.¹ Piclidenoson (1 and 3 mg/kg) also reduces colonic inflammatory cell infiltration and damage in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250) and in IL-10^-/- mice.³

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1. Jacobson, K.A., Merighi, S., Varani, K., et al. A₃ adenosine receptors as modulators of inflammation: From medicinal chemistry to therapy. Med. Res. Rev. 38(4), 1031-1072 (2018).

2. Auchampach, J.A., Rizvi, A., Qiu, Y., et al. Selective activation of A₃ adenosine receptors with N6-(3-iodobenzyl)adenosine-5′-N-methyluronamide protects against myocardial stunning and infarction without hemodynamic changes in conscious rabbits. Circ. Res. 80(6), 800-809 (1997).

3. Mabley, J., Soriano, F., Pacher, P., et al. The adenosine A₃ receptor agonist, N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide, is protective in two murine models of colitis. Eur. J. Pharmacol. 466(3), 323-329 (2003).