药物处置incadronate,新二磷酸盐有骨转移的老鼠。

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臼井仪人T,田中年代,Sonoda T,小泽Y,寺K,中村E,渡边T, Higuchi年代

药物处置incadronate,新二磷酸盐有骨转移的老鼠。

Xenobiotica。1997年5月,27 (5):479 - 87。doi: 10.1080 / 004982597240442。

PubMed ID
9179988 (在PubMed
]
文摘

1。药物处置incadronate裸体鼠与骨转移引起的静脉注射后人类黑色素瘤A375细胞进行了研究。2。incadronate的药物动力学(等离子体浓度、尿尿蛋白和骨吸收与骨转移鼠没有明显区别,但是在控制老鼠。然而,这种化合物是有选择地采取骨转移性肿瘤周边地区的巢穴。3所示。药物浓度在骨肿瘤巢周边地区3 - 10微克/克,这些水平高于IC50(0.35微克/毫升)的抑制作用,这种药物在体外破骨细胞。4所示。相反,浓度在肿瘤巢本身是< 0.7微克/克,明显低于IC50(35微克/毫升)对肿瘤细胞的增殖抑制作用在体外。5。 These results strongly suggest that pharmacological action of incadronate in mouse with bone metastases (inhibitory effect on the growth of metastatic tumour in bone) is caused not by the direct action on the tumour cells but by the distribution of the drug in the perifocal bone region followed by inhibition of the activity of osteoclasts, resulting in inhibition of the osteolytic process, which is necessary for the progress of metastatic tumour.

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