| Bioactivity | RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7)[1]. | ||||||||||||
| Target | pIC50: 5.9 (human homomultimeric P2X3 receptor); 7.0 (human heteromultimeric P2X2/3 receptor) | ||||||||||||
| In Vivo | In a guinea pig ureter-afferent nerve preparation, and mouse bladder-pelvic nerve preparation, RO-3 dose-dependently reduces afferent nerve activity induced by distension or α,β-meATP[1].RO-3 has activity in several rodent models of pain, as well as in cystometry models optimized to measure various parameters associated with sensory regulation of the micturition reflex[1].RO-3 has moderate to high metabolic stability in rat and human hepatocytes and liver microsomes, and is highly permeable, orally bioavailable (14%), and has a reasonable in vivo plasma half-life (t1/2=0.41 h) in rats[1]. | ||||||||||||
| Name | RO-3 | ||||||||||||
| CAS | 1026582-88-6 | ||||||||||||
| Formula | C16H22N4O2 | ||||||||||||
| Molar Mass | 302.37 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ford AP, et al. Purinoceptors as therapeutic targets for lower urinary tract dysfunction. Br J Pharmacol. 2006;147 Suppl 2(Suppl 2):S132-S143. |