坎利酮 商品名 Contaren, Luvion, Phanurane, Spiroletan 其他名称 Aldadiene;[ 1] SC-9376; RP-11614; 7α-Desthioacetyl-δ6 -spironolactone; 6,7-Dehydro-7α-desthioacetylspironolactone; 17-Hydroxy-3-oxo-17α-pregna-4,6-diene-21-carboxylic acid γ-lactone AHFS /Drugs.com 国际药品名称 药物类别 抗盐皮质激素 ATC码 血浆蛋白结合率 95% 生物半衰期 16.5 hours[ 2]
10,13-Dimethylspiro[2,8,9,11,12,14,15,16-octahydro-1H -cyclopenta[a ]phenanthrene-17,5'-oxolane]-2',3-dione
CAS号 976-71-6 N PubChem CID ChemSpider UNII ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.012.322 化学式 C 22 H 28 O 3 摩尔质量 340.46 g·mol−1 3D模型(JSmol )
O=C5\C=C4\C=C/[C@@H]1[C@H](CC[C@]3([C@H]1CC[C@]32OC(=O)CC2)C)[C@@]4(C)CC5
InChI=1S/C22H28O3/c1-20-9-5-15(23)13-14(20)3-4-16-17(20)6-10-21(2)18(16)7-11-22(21)12-8-19(24)25-22/h3-4,13,16-18H,5-12H2,1-2H3/t16-,17+,18+,20+,21+,22-/m1/s1
Y Key:UJVLDDZCTMKXJK-WNHSNXHDSA-N
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坎利酮 (英语:Canrenone ,商品名有:Contaren、Luvion、Phanurane、Spiroletan等),别名坎利酸内酯 或烯睾丙内酯 。是一种有机化合物 ,分子式为C22 H28 O3 ,属于甾体 类抗盐皮质激素 [ 3] [ 4] ,临床上可用作醛固酮 拮抗剂治疗水肿 、心衰 、高血压 、肝腹水 等疾病[ 5] ,在意大利 、比利时 等国也用作利尿剂 [ 6] [ 7] [ 8] [ 9] ,同时也是螺内酯 的活性代谢产物 [ 10] [ 2] 。坎利酮可被赭曲霉 等微生物发酵作用对11号碳进行羟基化 ,得到11α-羟基坎利酮 [ 11] [ 5] 。坎利酮同时也是螺内酯和依普利酮 的原料[ 12] 。
坎利酮抗盐皮质激素作用比螺内酯强,但抗雄激素 作用要弱于螺内酯[ 13] [ 14] ,不过利用其抗雄激素作用可用于治疗女性多毛症 [ 15] 。作为利尿剂,螺内酯转化成系列代谢产物后,坎利酮贡献了约10-25%的保钾利尿作用 ,7α-硫代甲基螺内酯 则主要贡献了约80%[ 16] [ 17] [ 18] 。
坎利酸
参考文献
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