- 概述
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。
- 生物活性
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。
- 靶点
IC50: antifungal
- 体内研究
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.
Animal Model:
BALB/c mice
Dosage:
0.3%-3% dosage
Administration:
Treatment for ear
Result:
Exhibited an inhibition effect of LCZ on ear swelling induced by topical application of TPA in mice.
Animal Model:
Four week old C57BL/6 mice infected intraperitoneally with LP-BM5 murine leukaemia virus
Dosage:
3, 10 or 30 mg/kg
Administration:
Oral adminstration
Result:
Inhibited
C. neoformans
growth in both normal and
C. neoformans
-induced encephalitis MAIDS mice .
- 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。
- 抗真菌药。在临床研究中。
