Applicationof a Simple Competitive Protein-bindingAssay Technique to the Pharmacokineticsof N-(Phosphonacetyl)-L-aspartatein Humans
Applicationof a Simple Competitive Protein-bindingAssay Technique to the Pharmacokineticsof N-(Phosphonacetyl)-L-aspartatein Humans
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简单的竞争性蛋白质结合测定技术在人体 N-(膦乙酰基)-L-天冬氨酸药代动力学中的应用
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发表时间：
1980
期刊：
影响因子：
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通讯作者：
B. Chabner
中科院分区：
文献类型：
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作者：
C. Erlichman;J. Strong;B. Chabner
PALA，其基于通过将复合物粘附到硝酸纤维素过滤器上来分离结合和游离PALA。该试验已用于PALA I期和II期试验的初步药代动力学研究。此外，该方法允许定量的结合动力学的PALA和它的目标酶。材料和方法材料。未标记的PALA从国家癌症研究所药物开发处获得。PALA（比活度，23 mCi/mmol）获自斯坦福大学研究所，门洛帕克，加利福尼亚州。放射自显影和31 P核磁共振检测的[14 C]PALA纯度分别为97%和98%。[14 C]PALA的高压液相色谱法得到95%纯度的化合物。咪唑、EDTA和2-巯基乙醇为标准试剂级。
PALA which is based on the separation of bound and free PALA by adherence of the complex to nitrocellulose filters. This assayhas been used in preliminary pharmacokineticstud ies during Phase I and II trials of PALA. Furthermore, this methodallows quantitation of the binding kinetics of PALAand its target enzyme. MATERIALS AND METHODS Materials. Unlabeled PALA was obtained from the Drug DevelopmentBranch of the National Cancer Institute. [‘4CJ PALA (specific activity, 23 mCi/mmol) was obtained from the Stanford ResearchInstitute, Menlo Park, Calif. The [‘4C]PALA was 97% pure by radioautography and 98% pure by 31P nuclear magnetic resonance. High-pressure liquid chromatog raphy of the [‘4C]PALA yielded 95% pure compound. lmidaz ole, EDTA, and 2-mercaptoethanol were of standard reagent grade.