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首页> 外文期刊>Journal of pharmaceutical sciences. >Bisphosphonate action: revelations and deceptions from in vitro studies.
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Bisphosphonate action: revelations and deceptions from in vitro studies.

机译：双膦酸盐的作用：体外研究的启示和欺骗。

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Bisphosphonates (BPs) are a class of drugs used in the treatment of osteoporosis and diseases of high bone turnover, as well as for control of skeletal related events secondary to malignant disease. The key to BP specificity is their capacity to bind rapidly and with high affinity to bone surfaces. The cellular targets of BPs at the bone surface have been a source of controversy. In addition to osteoclasts, it has been frequently proposed that BPs may affect a variety of cell types including osteoclast precursors, osteoblasts and bone-lining cells, immunogenic cells, and tumour cells. However, there is an emerging body of literature from in vitro studies indicating that BPs are only released and taken up from bone surfaces by resorbing osteoclasts. In this scenario, the only significant exposure of non-resorbing cells to BP would occur during the initial period after dosing, prior to drug clearance from the soft tissues. Auspiciously, several groups have reported on revised culture systems that better reflect the pharmacology of BP dosing.
机译：双膦酸盐（BPs）是一类药物，用于治疗骨质疏松症和高骨转换率疾病，以及用于控制继发于恶性疾病的骨骼相关事件。 BP特异性的关键在于它们快速结合骨表面的亲和力。 BP在骨表面的细胞靶点一直是引起争议的原因。除破骨细胞外，经常提出BP可能影响多种细胞类型，包括破骨细胞前体，成骨细胞和骨衬细胞，免疫原性细胞和肿瘤细胞。然而，来自体外研究的新兴文献表明，BP仅通过吸收破骨细胞而从骨表面释放并吸收。在这种情况下，非吸收性细胞对BP的唯一显着暴露将发生在给药后的最初阶段，即从软组织清除药物之前。幸运的是，几个小组已经报告了改良的培养系统，可以更好地反映BP剂量的药理学。

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