131631-89-5
131631-89-5 结构式
基本信息
N-[3-[4-[[4-(3,4-二氢-2-氧代-1(2H)-喹啉基)-1-哌啶基]羰基]苯氧基]丙基]乙酰胺
Fuscoside
OPC 21268
OPC-21268 hydrate
OPC 21268
OPC-21268
OPC21268
1-[1-[4-(3-Acetylaminopropoxy)benzoyl]-4-piperidyl]-3,4-dihydroquinolin-2(1H)-one
1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate
N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide
N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide
Acetamide, N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-
物理化学性质
常见问题列表
IC50: 0.4 μM (vasopressin V1)
Ki: 0.14 μM (vasopressin V1)
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).
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.