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- W3030906636 abstract "ObjectiveTo explore a PET probe, 11C-GF120918 in the assessing of the function and significance of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) .MethodsThe mice were injected with chemically synthesized 11C-GF120918. An automatic gamma counter was used to measure the 11C-GF120918 radiation intensity of the various organs of the mice at different times and dosages. Simultaneously, HPLC was employed to detect the metabolism of 11C-GF120918 in the brain and blood of the mice. The four mice groups, namely, P-gp knockdown mice, BCRP knockdown mice, P-gp/BCRP knockdown mice, and wild mice, were manually injected with 11C-GF120918. The radiation intensity of 11C-GF120918 in the mice brain was detected by PET.ResultsAfter the 11C-GF120918 injection, the tissues and organs of mice were more widely distributed compared with those of the wild mice (χ2=8.14, P<0.05) . Thirty minutes after injection, the 11C-GF120918 radiation intensity in the brain and blood were still (99.3±0.5) % and (83.2±3.5) %, respectively, with better biochemistry and radiation stability. In PET studies, AUCbrain[0~60 min] in the P-gp knockout mice was nine times higher than that in the wild group (χ2=7.69, P<0.05) . The AUCbrain[0-60 min] of the BCPR knockout mice was three times higher than that in the wild group (χ2=8.24, P<0.05) . The evident effect of 11C-GF120918 was relatively stable.Conclusion11C-GF120918 can be used as PET probes to evaluate the multi-drug resistance of P-gp and BCRP.Key words: P-glycoprotein; Neoplasms; Positron-emission tomography; Breast cancer resistance protein" @default.
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- W3030906636 date "2016-01-25" @default.
- W3030906636 modified "2023-09-23" @default.
- W3030906636 title "Developing P-glycoprotein inhibitor marked by PET" @default.
- W3030906636 doi "https://doi.org/10.3760/cma.j.issn.1673-4114.2016.01.001" @default.
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