MRE 3008F20

MRE 3008F20 is an adenosine A₃ receptor antagonist (K_i = 0.8 nM for the human receptor).¹ It is selective for the adenosine A₃ receptor over adenosine A₁, -A_2A, and -A_2B receptors (K_is = 1,197, 140, and 2,056 nM, respectively, for the human receptors). MRE 3008F20 inhibits cAMP accumulation induced by IB-MECA (piclidenosan; Item No. 28445) in CHO cells expressing the human adenosine A₃ receptor (IC₅₀ = 5.2 nM). It reverses decreases in NF-κB activation and TNF-α and IL-8 levels induced by NECA (5’-N-ethylcarboxamidoadenosine; Item No. 21420) or 2-Cl-IB-MECA (Item No. 27336) in LPS-stimulated primary human osteoarthritic synoviocytes when used at a concentration of 1 µM.²

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1. Baraldi, P.G., Cacciari, B., Romagnoli, R., et al. Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A₃ adenosine receptor antagonists: influence of the chain at the N8 pyrazole nitrogen. J. Med. Chem. 43, 4768-4780 (2000).

2. Varani, K., Vincenzi, F., Tosi, A., et al. Expression and functional role of adenosine receptors in regulating inflammatory responses in human synoviocytes. Br. J. Pharmacol. 160(1), 101-115 (2010).