中文同义词:
3-氨基-1-羟基丙亚基-1,1-二磷酸;帕米膦酸及帕米膦酸钠;帕屈膦酸;3-氨基-1-羟基-1,1-丙烷二膦酸;帕米膦酸;(3-氨基-1-羟基亚丙基)双膦酸;伊班膦酸杂质5
英文同义词:
PAMIDRONIC ACID;PAMIDRONIC ACID SODIUM SALT;Rescriptor;amidronate;DLV;(3-amino-1-hydroxypropylidene)bisphosphonic acid;(3-Amino-1-hydroxypropylidene)diphosphonic acid;3-AMINO-1-HYDROXY-1,1-PROPANEDIPHOSPHONIC ACID
相关类别:
其它药物;药物;医药原料;(intermediate of pamidronate disodium);Delavirdine;API
储存条件
Keep in dark place,Inert atmosphere,2-8°C
生物活性
Pamidronic acid 是用于研究各种骨吸收类疾病的药物。
体外研究
Osteosarcoma cell viability decreases significantly in a concentration- and time-dependent manner at pamidronate concentrations ranging from 100 to 1000 μM, most consistently after 48 and 72 hours exposure. In treated osteosarcoma cells, the lowest percentage cell viability is 34% (detected after 72 hours exposure to 1000μM pamidronate). Pamidronate disodium inhibits Wnt and β-catenin signaling, which controls osteogenic differentiation in BMMSCs. Wnt3a, a Wnt and β-catenin signaling activator, reverses the negative effects caused by pamidronate disodium to salvage the osteogenic defect in BMMSCs.
体内研究
Pamidronic acid can significantly inhibit and even reverse early osteoarthritic subchondral bone loss, thus alleviating the process of cartilaginous degeneration. The mechanisms involved may be associated with the upregulation of OPG expression, and downregulation of RANKL, MMP-9 and TLR-4 expression.
化学性质
结晶，熔点227~229℃。
帕米膦酸二钠(Pamidronate Disodium)：C3H9NO7P2Na2?5H2O。[57248-88-1]。失水温度从77.5℃到239.31℃，失水量为24．65%。
用途
二膦酸类骨吸收抑制剂。用于肿瘤高血钙症、佩吉特氏病、恶性肿瘤及正常血钙的骨质溶解性骨转移、特发性骨质疏松症。疗效显著，副作用低。
生产方法
氯苯和β-氨基丙酸的水溶液加热至约100℃，搅拌下滴加三氯化磷，再保温反应。冷至室温，通氮气除去氯化氢气体。分出氯苯液，缓慢滴加水。搅拌升温至100℃反应。冷冻析晶，过滤，得帕米膦酸，收率68%，熔点227-229℃。
帕米膦酸悬浮于水，滴加30%氢氧化钠至Ph值7.2—7.4。-5-5℃冷置析晶，过滤。滤饼加适量蒸馏水，加热溶解，活性炭脱色，冷冻结晶，过滤，室温真空干燥至恒重，得帕米膦酸二钠五水合物，收率78.6%。
