Molecular Formula | C23H25IN2O3
|
Molar Mass | 504.36 |
Density | 1.49±0.1 g/cm3(Predicted) |
Boling Point | 605.9±55.0 °C(Predicted) |
Solubility | DMSO: >5mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 6.98±0.10(Predicted) |
Storage Condition | 2-8°C |
In vitro study | The AM251 and 6-Iodopravadoline (AM630)-evoked Ca 2+ influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC 50 for AM251 and 6-Iodopravadoline are 7.37 μM and 15.6 μM, respectively. AM251 and 6-Iodopravadoline activate TRPA1 in TG sensory neurons. 6-Iodopravadoline is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). AM251 and 6-Iodopravadoline activation of TRPA1 is modulated by TRPV1. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. 6-Iodopravadoline (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner. 6-Iodopravadoline (1 μM) blocks the CP-55,940 dose response with EC 50 of 170 nM at human and EC 50 of 110 nM at rat cannabinoid CB2 receptor. |
In vivo study | 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box compared with vehicle group. 6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used. |