Molecular Formula | C33H27NO8 |
Molar Mass | 565.57 |
Density | 1.46±0.1 g/cm3(Predicted) |
Boling Point | 840.4±65.0 °C(Predicted) |
Solubility | H2O: ~34mg/mL |
Appearance | powder |
Color | white |
pKa | 2.57±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | A- 317491 effectively inhibited recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM), compared with other P2 receptors and neurotransmitter receptors, ion channels and enzymes (IC50 >10 M), with high selectivity for P2X3 and P2X2/3 receptors. No detectable metabolic processes (oxidation or glycolipidation) occurred in A- 317491 of human and rat hepatocyte microsomes in vitro. |
In vivo study | In rats, A- 317491(ED50=30 μmol/kg s.c.) was able to dose-dependently reduce CFA(complete Freund's adjuvant)-induced thermal hyperalgesia. Thermal hyperalgesia and mechanical hyperalgesia (ED50=10-15 μmol/kg s.c.) were effectively relieved by A- 317491 after chronic neuroconstriction injury. A- 317491 is active in chronic pain models, but in acute pain, postoperative pain, visceral pain, there was no nociceptive effect (ED50 >100 μmol/kg s.c.). Preliminary pharmacokinetic studies in rats showed high systemic bioavailability A- 317491 after subcutaneous injection of 10 μmol/kg A- 317491, plasma concentration is approximately 15 μg/ml,>99% protein binding, half-life in plasma is 11 hours. Systemic administration (A-317491) was effective in reducing pain-related behaviors in several animal models of inflammatory, neuropathic pain. A- 317491 was found not to be significantly involved in the central nervous system in the current study. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.768 ml | 8.841 ml | 17.681 ml |
5 mM | 0.354 ml | 1.768 ml | 3.536 ml |
10 mM | 0.177 ml | 0.884 ml | 1.768 ml |
5 mM | 0.035 ml | 0.177 ml | 0.354 ml |