OPC 21268

OPC-21268 is a vasopressin 1 receptor antagonist potentially for the treatment of heart failure and hypertension. (In Vitro) :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) . (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. 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.

131631-89-5

OPC-21268 | OPC21268 | OPC 21268

>98% (HPLC)

DMSO : 50 mg/mL. 111.22 mM

CC (=O) NCCCOC1=CC=C (C=C1) C (=O) N2CCC (CC2) N3C (=O) CCC4=CC=CC=C43

C26H31N3O4

449.55

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.