Adenosine A2 receptor agonists,potent and selective
CAS：120225-54-9
分子式：C23H29N7O6
分子量：499.52
纯度：98%
存储：Store at -20°C

Background:

CGS 21680 is a selective agonists of A2 adenosine receptor with IC50 value of 22nM [1].

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 [1].

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 [2].

参考文献:
[1] Alan J. Hutchison, Randy L. Webb, Howard H. Oei, Geetha R. Ghai, Mark B. Zimmerman and Michael Williams. CGS 21680C, an A2 Selective Adenosine Receptor Agonist with Preferential Hypotensive Activity. The Journal of Pharmacology and Experimental Therapeutics. 1989, 25 (1): 47-55.
[2] Daniela Impellizzeri, Rosanna Di Paola, Emanuela Esposito, Emanuela Mazzon, Irene Paterniti, Alessia Melani, Placido Bramanti, Felicita Pedata, Salvatore Cuzzocrea. CGS 21680, an agonist of the adenosine (A2A) receptor, decreases acute lung inflammation. European Journal of Pharmacology. 2011, 68: 305-316.