中文名 | 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 |
英文名 | OPC 21268 |
别名 | 化合物OPC 21268 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 |
英文别名 | OPC21268 OPC-21268 OPC 21268 OPC-21268 hydrate 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 N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate |
CAS | 131631-89-5 |
化学式 | C26H31N3O4 |
分子量 | 449.54 |
密度 | 1?+-.0.06 g/cm3(Predicted) |
沸点 | 772.5±60.0 °C(Predicted) |
溶解度 | DMSO: ≥ 20 mg/mL |
酸度系数 | 16.17±0.46(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to off-white |
体外研究 | 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). |
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. |
危险品标志 | Xn - 有害物品 N - 危害环境的物品 |
风险术语 | R22 - 吞食有害。 R50 - 对水生生物有极高毒性。 |
安全术语 | 61 - 避免释放至环境中。参考特别说明/安全数据说明书。 |
危险品运输编号 | UN 3077 9 / PGIII |
WGK Germany | 3 |
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