AB-MECA

AB-MECA is an adenosine A₃ receptor agonist (K_i = 430.5 nM for the human receptor expressed in CHO cells).¹ It inhibits LPS-induced TNF-α production in primary cultured human lung macrophages (pD₂ = 6.9).² AB-MECA increases contraction of isolated guinea pig trachea ex vivo when used at a concentration of 0.1 μM and increases bronchoconstriction in vivo when administered at a dose of 3 μg/kg in a guinea pig model of ovalbumin-sensitized asthma.³ A radiolabeled form of AB-MECA has been used for radioligand binding assays and binds to rat adenosine A₁ and A₃ receptors (K_ds = 3.42 and 1.48 nM in COS-7 and CHO cells, respectively) and canine adenosine A_2a receptors (K_d = 25.1 nM in COS-7 cells).⁴

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1. Yates, L., Clark, J.H., Martin, T.J., et al. Radioligand binding and functional responses of ligands for human recombinant adenosine A₃ receptors. Auton. Autacoid Pharmacol. 26(2), 191-200 (2006).

2. Buenestado, A., Grassin Delyle, S., Arnould, I., et al. The role of adenosine receptors in regulating production of tumour necrosis factor-α and chemokines by human lung macrophages. Br. J. Pharmacol. 159(6), 1304-1311 (2010).

3. Mikus, E.G., Szeredi, J., Boer, K., et al. Evaluation of SSR161421, a novel orally active adenosine A₃ receptor antagonist on pharmacology models. Eur. J. Pharmacol. 699(1-3), 172-179 (2013).

4. Olah, M.E., Gallo-Rodriguez, C., Jacobson, K.A., et al. 125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A₃ adenosine receptor. Mol. Pharmacol. 45(5), 978-982 (1994).