Name | RO3 |
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Synonyms |
RO3
5-(2-Isopropyl-4,5-dimethoxybenzyl)pyrimidine-2,4-diamine 5-(2-Isopropyl-4,5-dimethoxybenzyl)-2,4-pyrimidinediamine 2,4-Pyrimidinediamine, 5-[[4,5-dimethoxy-2-(1-methylethyl)phenyl]methyl]- |
Description | 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]. |
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Related Catalog | |
Target |
pIC50: 5.9 (human homomultimeric P2X3 receptor); 7.0 (human heteromultimeric P2X2/3 receptor)[1] |
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]. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 516.3±60.0 °C at 760 mmHg |
Molecular Formula | C16H22N4O2 |
Molecular Weight | 302.371 |
Flash Point | 266.1±32.9 °C |
Exact Mass | 302.174286 |
LogP | 2.43 |
Vapour Pressure | 0.0±1.3 mmHg at 25°C |
Index of Refraction | 1.596 |