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Enhancement of cellular gallium uptake

机译:增强细胞对镓的摄取

摘要

A method for improving cellular gallium uptake (particularly of tumor cells) by exposing cells to a nifedipine photodegradation product, or an analog thereof. In particular embodiments, the gallium uptake enhancer is selected from the group of A-B and formula (I), wherein A is a pyridine and B is a nitrosophenyl, and n=1-10. In yet other embodiments, the uptake enhancer is formula (II), wherein R1-9 are independently selected from the group consisting of H, halogen, haloalkyl, NO2, NO, SO2, a C1-6 alkyl, a COOR10 wherein R10 is H or C1-6 alkyl, and an —OR11 wherein R11 is H or C1-6 alkyl; wherein at least one of R5 and R7 is NO. The uptake enhancers are particularly useful in imaging tumors, using such techniques as gallium scanning, in which the dose of the gallium isotope can be decreased or its imaging efficiency improved. Alternatively, the method can be used to improve efficacy of gallium containing chemotherapeutic regiments in the treatment of tumors and hypercalcemia, or to improve the uptake of other chemotherapeutics that use a similar transferrin independent uptake mechanism. embedded image
机译:一种通过使细胞暴露于硝苯地平光降解产物或其类似物来改善细胞镓(尤其是肿瘤细胞)摄取的方法。在特定的实施方案中,镓吸收增强剂选自A-B和式(I)的组,其中A为吡啶且B为亚硝基苯基,且n等于1-10。在其他实施方案中,摄取增强剂是式(II),其中R 1-9 独立地选自H,卤素,卤代烷基,NO 2 , NO,SO 2 ,C1-6烷基,COOR 10 (其中R 10 是H或C1-6烷基)和&m; OR 11 ,其中R 11 是H或C1-6烷基;其中R 5 和R 7 中的至少一个为NO。使用诸如镓扫描的技术,摄取增强剂在使肿瘤成像中特别有用,其中可以减少镓同位素的剂量或提高其成像效率。或者,该方法可用于改善含镓化疗方案在治疗肿瘤和高钙血症中的功效,或改善使用类似转铁蛋白独立摄取机制的其他化疗药物的摄取。 “嵌入式图像”

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