Objective: In this study we investigated the effect of CGS 21680 (2-p-(2-Carboxyethyl)phenethylamino-5-N-ethylcarboxamidoadenosine hydrochloride), an adenosine A2A receptor agonist, in a model of dextran sulphate sodium (DSS)-induced colitis. Methods: NMRI mice were fed 5 % (w/v) DSS, and were treated intraperitoneally with 0.5 mg/kg CGS 21680 or vehicle for 10 days. Changes of bodyweight, colon length, the incidence of rectal bleeding, levels of macrophage inflammatory protein (MIP)-1α, MIP-2, interferon γ, interleukin (IL)-1β, IL-12 and tumour necrosis factor-α from homogenates of colon biopsies, and the release of [ 3H]acetylcholine (ACh) from longitudinal muscle strip were determined. Results: DSS significantly decreased bodyweight, colon length, and it increased the incidence of rectal bleeding and levels of MIP-1α, MIP-2 and IL-1β compared to DSS-untreated animals. CGS 21680 had no effect on these changes. No change could be observed in release of ACh in DSS-induced colitis with or without CGS 21680. Conclusion: In summary, CGS 21680 is ineffective in ameliorating DSS-induced colitis in mice.
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