2-Cl-IB-MECA

2-Cl-IB-MECA (Chloro-IB-MECA, CF-102, Namodenoson) is a potent, selective A3 adenosine receptor agonist with Ki of 0.33 nM, 2500- and 1400-fold selectivity over A1 and A2a receptors; also displays 46,000-fold selectivity versus the Na (+) -independent adenosine transporter; inhibits adenylate cyclase via rat A3 receptors in CHO cells (IC50=67 nM) ; induces apoptosis in HL-60 cells at concentrations of <30 uM, significantly induced Ca (2+) release from intracellular Ca (2+) pools followed by Ca (2+) influx; increases plasma histamine concentrations in conscious rats.Liver Cancer Phase 2 Clinical (In Vitro) :In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions. High concentrations of Namodenoson (2-Cl-IB-MECA) directly cause influx of Ca2+. (In Vivo) :Intravenous administration of 200 μg/kg Namodenoson (2-Cl-IB-MECA) resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of Namodenoson (2-Cl-IB-MECA) did not elicit any hemodynamic effects.