Background:

Capadenoson is a selective agonist of Adenosine A1 receptor [1].
Adenosine A1 receptor is a member of G-protein coupled receptor 1 family and plays an important role in the fertilization process, kidney function and ethanol intoxication. Many studies have shown that Adenosine A1 receptor is correlated with a variety of diseases, like angina, heart failure, and its agonist is becoming a promising target in clinic [1].
Capadenoson is a potent Adenosine A1 receptor agonist and belongs to the non-nucleosidic adenosine receptor family. When tested with perfused rat hearts isolated from Wista and SHR strains, capadenoson combined with CCPA treatment significantly decreased NE release in a dose-dependent manner [1].
In dog model with heart failure induced by microembolization, oral administration of capadenoson for 12 weeks improved left ventricular function and prevented progressive remodeling [2]. When pre-treated Wistar rats with capadenoson (0.15 mg/kg) for 5 days, physical restraint for 2 hours increased heart rate [1].
When tested with male patients with stable angina, oral administration of capadenoson lowered exercise heart failure at comparable maximum workload [3].
参考文献:
[1].Bott-Flugel, L., et al., Selective attenuation of norepinephrine release and stress-induced heart rate increase by partial adenosine A1 agonism. PLoS One, 2011. 6(3): p. e18048.
[2].Sabbah, H.N., et al., Chronic therapy with a partial adenosine A1-receptor agonist improves left ventricular function and remodeling in dogs with advanced heart failure. Circ Heart Fail, 2013. 6(3): p. 563-71.
[3].Tendera, M., et al., The new oral adenosine A1 receptor agonist capadenoson in male patients with stable angina. Clin Res Cardiol, 2012. 101(7): p. 585-91.