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RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).1 It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
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1. Purinoceptors as therapeutic targets for lower urinary tract dysfunction. Br. J. Pharmacol. 147(Suppl. 2), S132-S143 (2006).