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

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

中文名称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
中文同义词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;化合物OPC 21268;OPC 21268,加压素V1拮抗剂
英文名称OPC 21268
英文同义词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-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate;OPC-21268 hydrate;N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide;OPC 21268;N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide;OPC 21268;OPC-21268;OPC21268
CAS号131631-89-5
分子式C26H31N3O4
分子量449.54
EINECS号
相关类别
Mol文件131631-89-5.mol
结构式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 结构式

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 性质

沸点772.5±60.0 °C(Predicted)
密度1?+-.0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度二甲基亚砜:≥20mg/mL
酸度系数(pKa)16.17±0.46(Predicted)
形态粉末
颜色白色至类白色

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 用途与合成方法

Fuscoside (OPC-21268) 是一种口服有效的非多肽类加压素受体 (vasopressin V1) 拮抗剂, IC50 值为0.4 μM。

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.

安全信息

危险品标志Xn,N
危险类别码22-50
安全说明61
危险品运输编号UN 3077 9 / PGIII
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-15009Fuscoside1 mg377元
2024/04/30HY-15009N-[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
131631-89-55mg900元

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 上下游产品信息

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