| 靶点: |
IC50: 0.4 μM (vasopressin V1);Ki: 0.14 μM (vasopressin V1) |
| 体内研究: |
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. |
| 参考文献: |
1. Yamamura Y, et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science. 1991 Apr 26;252(5005):572-4. 2. Bemana I, et al. Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats. Neurosurgery. 1999 Jan;44(1):148-54. |
| 溶解性: |
DMSO: ≥20mg/mL |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
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1mg |
5mg |
10mg |
| 1 mM |
0 ml |
0 ml |
0 ml |
| 5 mM |
0 ml |
0 ml |
0 ml |
| 10 mM |
0 ml |
0 ml |
0 ml |
| 50 mM |
0 ml |
0 ml |
0 ml |
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| 注意: |
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