GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

A3:1070 nM(Ki, human), A1:1940 nM(Ki, human), A2B:22 nM(Ki, human), A2A:3280 nM(Ki, human)

GS-6201 (2 mg/kg; p.o.) treatment displays the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively [1]. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) obviously decreases IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) causes an obvious attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days [2].