拉诺康唑为咪唑类抗真菌药物,作用机制同其他咪唑类药物,主要通过抑制14-甲基羊毛甾醇的脱14-甲基阶段,从而达到抑制真菌细胞麦角固醇合成的目的而具有抗真菌作用。
Lanoconazole 是一种强效口服咪唑类抗真菌 (antifungal) 试剂,具有广谱的体内外抗真菌活性。Lanoconazole 通过抑制 sterol 14-alpha 去甲基酶,阻断真菌膜上的 ergosterol 生物合成,从而干扰 ergosterol 的生物合成。Lanoconazole 可用于皮肤真菌病和甲真菌病的研究。
Lanoconazole (treatment for ear; 0.3%-3%; 6 days) dose‐dependently suppressesTPA-induced irritant dermatitis, suppresses the production of neutrophil chemotactic factors such as keratinocyte‐derived chemokine and macrophage inflammatory protein‐2, and inhibited neutrophil infiltration to the inflammation site.Lanoconazole (oral administration; 3, 10 or 30 mg/kg; once a day; 3 weeks) significantly inhibits
C. neoformans
compared with the saline control in normal mice. In addtion, it significantly reduces the growth of
C. neoformans
in the lungs and brains of MAIDS mice.
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Animal Model:
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BALB/c mice
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Dosage:
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0.3%-3% dosage
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Administration:
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Treatment for ear
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Result:
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Exhibited an inhibition effect of LCZ on ear swelling induced by topical application of TPA in mice.
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Animal Model:
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Four week old C57BL/6 mice infected intraperitoneally with LP-BM5 murine leukaemia virus
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Dosage:
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3, 10 or 30 mg/kg
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Administration:
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Oral adminstration
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Result:
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Inhibited
C. neoformans
growth in both normal and
C. neoformans
-induced encephalitis MAIDS mice .
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化学性质
淡黄色结晶。熔点141.5℃。急性毒性LD
50雄、雌小鼠,雄、雌大鼠(mg/kg):3224,2715,993,652口服;2158,1743,1655,2596腹腔注射;全部>5000皮下注射。急性毒性LD
50大鼠致死量:>5000mg/kg。
用途
抗真菌药。在临床研究中。
生产方法
2-(1-咪唑基)乙腈与二硫化碳和氢氧化钾在二甲基甲酰胺中反应得连二硫酸酯的二钾盐,然后和1-(2-氯苯基)-1,2-二(甲磺酰氧基)乙烷环合。经硅胶柱层析分离(E)和(Z)异构体,而得拉诺康唑。