CGS 21680 is a selective agonists of A2 adenosine receptor with IC50 value of 22nM .
CGS 21680 is found to be potent and selective adenosine A2 receptor agonists. In a radioligand binding in vitro assay, CGS 21680 binds A2 receptor with IC50 value of 22nM and the A1/A2 ratio is 141, In the perfused rat heart model, CGS 21680 can increase coronary flow with greater EC25 value than 1000nM. It shows a good separation between its ability to induce vasorelaxation and bradycardia. CGS 21680 also has potent effect on blood pressure in vivo with EC25 value of 9µg/kg and it can induce an increase in heart rate .
It is reported that CGS 21680 also has the potency of anti-inflammatory. It can reduce the development of acute lung inflammation in a mouse model of carrageenan-induced pleurisy. In both prior and post-treatment, CGS 21680 can reduce the number of inflammatory cells and the degree of lung injury .