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坎利酮

坎利酮用途

Canrenone (Aldadiene; SC9376; SC14266) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。

坎利酮名称

[ CAS 号 ]:
976-71-6

[ 中文名 ]:
坎利酮

[ 英文名 ]:
Canrenone

[中文别名 ]:

6-去氢睾(甾)酮-17α-丙酸-γ-内酯

[英文别名 ]:

Phanurane
Luvion
ALDADIENE
Canrenone
Contaren
6-Dehydrotestosterone-17a-propionic Acid g-Lactone
CANRENONE-D4
11614 R.P.

坎利酮生物活性

[ 描述 ]:

Canrenone (Aldadiene; SC9376; SC14266) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 盐皮质激素受体

研究领域 >> 心血管疾病

[ 靶点 ]

Target: Aldosterone[1]

[体外研究]

Canrenone以剂量依赖的方式抑制eortieosterone,18-羟基去氧皮质酮,18-羟基皮质酮和醛固酮的产生[1]。 Canrenone剂量依赖性地减少血小板衍生的生长因子诱导的细胞增殖和运动。 Canrenone抑制血小板衍生生长因子诱导的Na +/H +交换蛋白1的活性[2]。

[体内研究]

Canrenone是大鼠中螺内酯的主要活性代谢产物,仅在一段有限的时间内。在慢性治疗期间,螺内酯和坎利酮对RAAS的作用之间出现差异,表明Canrenone的抗盐皮质激素活性降低,并且螺内酯的功效增加[3]。

[细胞实验]

将汇合的肝星状细胞（HSC）在SFIF培养基中温育24小时，并暴露于递增浓度的坎利酮（1,5,10,25μM）。在24-48小时培养期结束时通过台盼蓝染料排除试验评估细胞活力[2]。

[动物实验]

将大鼠[3] Canrenone（CAN）以两种不同剂量（10.25,20.5mg / mL）口服给予雄性SPF Sprague-Dawley大鼠6周。为了确定Na +，K +，液体和醛固酮的排泄，在每周的时间间隔收集6周后注定要杀死的大鼠的尿液[3]。

[参考文献]

[1]. Erbler HC, et al. On the mechanism of the inhibitory action of the spirolactone SC 9376 (aldadiene) on the production of corticosteroids in rat adrenals in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1973;277(2):139-49.

[2]. Caligiuri A, et al. Antifibrogenic effects of canrenone, an antialdosteronic drug, on human hepatic stellate cells. Gastroenterology. 2003 Feb;124(2):504-20.

[3]. Erbler HC, et al. Effect of spironolactone and its main metabolite canrenone on the renin-angiotensin-aldosterone-system during long-term treatment in rats. Acta Endocrinol (Copenh). 1979 Jan;90(1):147-56.

[相关活性小分子]

坎利酮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
541.1±50.0 °C at 760 mmHg

[ 熔点 ]:
158-160ºC

[ 分子式 ]:
C₂₂H₂₈O₃

[ 分子量 ]:
340.456

[ 闪点 ]:
237.6±30.2 °C

[ 精确质量 ]:
340.203857

[ PSA ]:
43.37000

[ LogP ]:
2.99

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.581

[ 储存条件 ]:
室温，干燥

坎利酮MSDS

坎利酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TU3493000

CHEMICAL NAME :: Pregna-4,6-diene-21-carboxylic acid, 17-hydroxy-3-oxo-, gamma-lactone, (17-alpha)-

CAS REGISTRY NUMBER :: 976-71-6

BEILSTEIN REFERENCE NO. :: 0046602

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C22-H28-O3

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ATDAEI Acute Toxicity Data. Journal of the American College of Toxicology, Part B. (Mary Ann Liebert, Inc., 1651 Third Ave., New York, NY 10128) V.1- 1990- Volume(issue)/page/year: 1,36,1990

坎利酮安全信息

[ 符号 ]:

GHS08, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H351-H411

[ 警示性声明 ]:
P280

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
40-51/53

[ 安全声明 (欧洲) ]:
36/37-61

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ 海关编码 ]:
29329990

坎利酮合成路线

坎利酮上下游产品

坎利酮上游产品

坎利酮下游产品

坎利酮文献

Aldosterone receptor blockers spironolactone and canrenone: two multivalent drugs.

Expert Opin. Pharmacother. 15(7) , 909-12, (2014)

Canrenone is a derivative of spironolactone with lower antiandrogen activity. The drug is used only in few countries and can block all the side effects of aldosterone (ALDO). The drug is effective eve...

Additional use of an aldosterone antagonist in patients with mild to moderate chronic heart failure: a systematic review and meta-analysis.

Br. J. Clin. Pharmacol. 75(5) , 1202-12, (2013)

Aldosterone antagonists (AldoAs) have been used to treat severe chronic heart failure (CHF). There is uncertainty regarding the efficacy of using AldoAs in mild to moderate CHF with New York Heart Ass...

The effects of canrenone on inflammatory markers in patients with metabolic syndrome.

Ann. Med. 47(1) , 47-52, (2015)

To evaluate the effects of canrenone compared to placebo on blood pressure control, some non-conventional biomarkers in cardiovascular stratification, and on metalloproteinases in patients affected by...

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坎利酮