An adenosine A3 receptor agonist
IB-MECA is an agonist of the adenosine A3 receptor with EC50 values of 0.11 uM. IC50 value: 0.11 uM (EC50) [3]Target: adenosine A3 receptorin vitro: IB-MECA has been shown to play important roles in cell proliferation and apoptosis in a variety of cancer cell lines. TheIB-MECA was capable of decreasing intracellular cyclic adenosine monophosphate (cAMP) that was the reason for the presence of functional A3 adenosine receptor on the cell lines. IB-MECA significantly reduced cell viability in a dose-dependent manner. IB-MECA, an A3AR agonist, inhibits the growth of different cancer cell types like melanoma, colon, breast, leukemia, and prostateIB-MECA was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 0.82 uM in OVCAR-3 cells. IB-MECA was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 1.2 uM in Caov-4 cells.in vivo: Administrations of single intraperitoneal doses of either IB-MECA 0.5 h post-irradiation resulted in statistically significant increases of MST in comparison with the control irradiated mice.[2]
参考文献:
[1]. Hofer M, et al. Agonist of the adenosine A3 receptor, IB-MECA, and inhibitor of cyclooxygenase-2, meloxicam, given alone or in a combination early after total body irradiation enhance survival of γ-irradiated mice. Radiat Environ Biophys. 2014 Mar;53(1):2
[2]. Abedi H, et al. Mitochondrial and caspase pathways are involved in the induction of apoptosis by IB-MECA in ovarian cancer cell lines. Tumour Biol. 2014 Nov;35(11):11027-11039.
[3]. Shin Y, et al. Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors Drug Dev Res. 1996 Sep 1;39(1):36-46.
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