Adenosine A2A receptor stimulation increases angiogenesis by down-regulating production of the antiangiogenic matrix protein thrombospondin 1.

Topical adenosine A2A receptor agonists promote wound healing by, among other effects, increasing microvessel formation. Results of representational display analysis of human umbilical vein endothelial cells suggested that A2A receptor occupancy modulates expression of the antiangiogenic matrix protein thrombospondin 1 (TSP1). We therefore determined whether A2A receptor occupation stimulates angiogenesis by modulating TSP1 secretion.

Adenosine A2A receptor agonists promote more rapid wound healing than recombinant human platelet-derived growth factor (Becaplermin gel).

Animal studies of the topical application of adenosine A2A receptor agonists show that it promotes wound closure. To further confirm the efficacy of adenosine A2A receptor agonists as promoters of wound healing, we compared the effect of MRE0094, a novel selective adenosine A2A receptor agonist, to CGS-21680, a reference selective adenosine A2A receptor agonist, as well as to recombinant human platelet-derived growth factor (0.01% Becaplermin gel), an agent currently used to promote healing of diabetic ulcers, on wound closure in healthy BALB/C mice.