| Bioactivity | Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. | ||||||||||||
| Target | IC50: 0.4 μM (vasopressin V1)Ki: 0.14 μM (vasopressin V1) | ||||||||||||
| Invitro | The concentration of Fuscoside (OPC-21268) that displaces 50% of specific AVP binding (IC50) is 0.4 μM for VI receptors and 100 μM for V2 receptors. The inhibition constant (Ki) of Fuscoside (OPC-21268) for V1 receptors (0.14 μM)[1]. | ||||||||||||
| In Vivo | 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[1]. 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[2]. | ||||||||||||
| Name | Fuscoside | ||||||||||||
| CAS | 131631-89-5 | ||||||||||||
| Formula | C26H31N3O4 | ||||||||||||
| Molar Mass | 449.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |