IB-MECA is an agonist of the adenosine A3 receptor with EC50 values of 0.11 μM. IB-MECA is a potent and selective A3adenosine receptor agonist with Ki value of 1.1, 54 and 56 nM for A3, A1 and A2A receptors, respectively, which possessing cardioprotective effect and reduces infarct size upon reperfusion in rats.
Adenosine receptors play an important role in cell growth and proliferation in different cell lines. The A3 adenosine receptor (A3AR) expression level in normal cells is low, while it is more highly expressed in various tumor cells. IB-MECA is a reversable A3AR agonist, inhibiting the growth of different cancer cell types like melanoma, colon, breast, leukemia, and prostate. IB-MECA was able to inhibit forskolin-stimulated cyclic adenosine monophosphate (cAMP) levels with EC50s of 0.82 μM and 1.2 μM in OVCAR-3 and Caov-4 ovarian cancer cells. Further, IB-MECA exhibited antiproliferative effect with IC50s of 32.14 μM and 45.37 μM for OVCAR-3 and Caov-4 ovarian cancer cells, respectively. 48 h treatment with IB-MECA induced apoptosis in those cell lines with dosage range 0.1-100 μM and significantly reduced cell viability in a dose-dependent manner with dosage range 0.0001-100 μM[3]. In B10CBAF1 male mice aged 3 months, IB-MECA (105 μg/kg) resulted in statistically significant increases of the mean survival time in comparison with the control irradiated mice[4].
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