依诺昔酮

依诺昔酮用途

Enoximone 是一种正性肌力血管舒张剂,也是一种选择性的,具有口服活性的磷酸二酯酶 III (PDE3) 抑制剂,IC50 为 5.9 μM。Enoximone 通过抑制 cGMP 抑制的 PDE 来诱导血管舒张并增加细胞内 cAMP 水平。Enoximone 还表现出 PDE4 抑制作用,对心肌 PDE4A 的 IC50 为 21.1 μM。Enoximone 可用于充血性心力衰竭的研究,并具有支气管扩张,抗哮喘和抗炎作用。

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依诺昔酮名称

[ CAS 号 ]:
77671-31-9

[ 中文名 ]:
依诺昔酮

[ 英文名 ]:
Enoximone

[中文别名 ]:

氢甲苯咪酮

[英文别名 ]:

Fenoximone
Enoximonum [Latin]
[14C]-Enoximone
Enoximona
MFCD00867130
Perfane
Enoximonum
Enoximona [Spanish]
Enoximone
Perfan

依诺昔酮生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

研究领域 >> 炎症/免疫

[ 靶点 ]

PDE3/PDE Ⅲ:5.9 μM (IC50)

PDE4A:21.1 μM (IC50, myocardial PDE4A)

[体外研究]

在体外,与稀释液处理的BAL嗜酸性粒细胞相比,10μM依诺西酮处理的支气管肺泡灌洗液(BAL)诱导的嗜酸性粒细胞CD11b表达明显降低[1]。

[体内研究]

局部应用依诺西酮(25μg；气管内给药)可消除屋尘螨(HDM)诱导的过敏性气道炎症[1]。依诺西酮治疗(25μg；持续5天)HDM暴露小鼠的炎症细胞数量显著减少,包括嗜酸性粒细胞、巨噬细胞、中性粒细胞、ILC2s和T细胞,表明依诺西酮治疗可减少气道炎症[1]。

[参考文献]

[1]. Jan Beute, et al. A Pathophysiological Role of PDE3 in Allergic Airway Inflammation. JCI Insight. 2018 Jan 25;3(2):e94888.

[2]. R C Dage, et al. Pharmacology and Pharmacokinetics of Enoximone. Cardiology. 1990;77 Suppl 3:2-13; discussion 27-33.

[3]. M B Vroom, et al. Effect of Phosphodiesterase Inhibitors on Human Arteries in Vitro. Br J Anaesth. 1996 Jan;76(1):122-9.

依诺昔酮物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 熔点 ]:
255-258°C

[ 分子式 ]:
C₁₂H₁₂N₂O₂S

[ 分子量 ]:
248.301

[ 精确质量 ]:
248.061951

[ PSA ]:
91.02000

[ LogP ]:
3.72

[ 外观性状 ]:
solid | light yellow

[ 折射率 ]:
1.645

[ 储存条件 ]:
Store at +4°C

[ 水溶解性 ]:
DMSO: 28 mg/mL, soluble

依诺昔酮MSDS

详细MSDS(安全技术说明书)

依诺昔酮安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;half-mask respirator (US);multi-purpose combination respirator cartridge (US)

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933290090

依诺昔酮合成路线

详细合成路线

依诺昔酮上下游产品

依诺昔酮上游产品

依诺昔酮下游产品

依诺昔酮制备

乙酰乙酸乙酯用亚硝酸作用后，再催化氢化得α-氨基乙酰乙酸乙酯，和异氰酸环合得咪唑环衍生物，氢氧化钠水溶液水解并脱羧，最后酰化得依诺昔酮。

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依诺昔酮海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

依诺昔酮文献

Recovery of heart function in children with acute severe heart failure.

Transplantation 85(7) , 975-9, (2008)

The prognosis of acute heart failure is such that many children are considered for transplantation. Recovery of severe heart failure in a proportion of patients diagnosed with either dilated cardiomyo...

Effects of enoximone on peripheral and central chemoreflex responses in humans.

Am. J. Physiol. Heart Circ. Physiol. 294(1) , H322-9, (2008)

cAMP plays an important role in peripheral chemoreflex function in animals. We tested the hypothesis that the phosphodiesterase inhibitor and inotropic medication enoximone increases peripheral chemor...

[Tolerance of enoximone in patients with heart failure].

Z. Kardiol. 80 Suppl 4 , 93-7, (1991)

Enoximone, a new phosphodiesterase-inhibitor with positive inotropic and vasodilating activities is available for intravenous use in patients with severe heart failure. A review of the current knowled...

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