Molecular Formula | C26H31N3O4 |
Molar Mass | 449.54 |
Density | 1?+-.0.06 g/cm3(Predicted) |
Boling Point | 772.5±60.0 °C(Predicted) |
Solubility | DMSO: ≥20mg/mL |
Appearance | powder |
Color | white to off-white |
pKa | 16.17±0.46(Predicted) |
Storage Condition | 2-8°C |
In vitro study | The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC 50 ) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (K i ) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM). |
In vivo study | Fuscoside (OPC-21268) competitively and specifically antagonizes pressor responses to AVP in vivo . Oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP in a dose- and time-dependent manner and the effect lasts for more than 8 hours at 30 mg/kg. Fuscoside (OPC-21268) predominantly exerts a protective effect in areas where the maximum amount of blood-brain barrier breakdown occurs, and it is effective in the treatment of cold-induced vasogenic brain edema. Fuscoside (OPC-21268) treatment at the dosages of 200 and 300 mg/kg significantly reduces brain water content in both hemispheres. Swelling of the traumatized hemispheres is also significantly reduced at 200 and 300 mg/kg dosages. |
Risk Codes | R22 - Harmful if swallowed R50 - Very Toxic to aquatic organisms |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |