MRE 3008F20

An adenosine A3 receptor antagonist (Ki = 0.8 nM for the human receptor), selective for the adenosine A3 receptor over adenosine A1, -A2A, and -A2B receptors (Kis = 1,197, 140, and 2,056 nM, respectively, for the human receptors), inhibits IB-MECA-induced cAMP accumulation in CHO cells expressing the human adenosine A3 receptor (IC50 = 5.2 nM), reverses NECA- or 2-Cl-IB-MECA-induced decreases in NF-kappaB activation and TNF-alpha and IL-8 levels in LPS-stimulated primary human osteoarthritic synoviocytes at 1 µM. Formulation: A solid. InChI: InChI=1S/C21H20N8O3/c1-3-10-28-12-15-17(26-28)24-20(25-21(30)22-13-6-8-14(31-2)9-7-13)29-19(15)23-18(27-29)16-5-4-11-32-16/h4-9,11-12H,3,10H2,1-2H3,(H2,22,24,25,26,30). InChIKey: CJRNHKSLHHWUAB-UHFFFAOYSA-N. SMILES: O=C(NC1=NC2=NN(CCC)C=C2C3=NC(C4=CC=CO4)=NN13)NC5=CC=C(C=C5)OC