P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain
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| Titel: | P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain |
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| Autoren: | Kyeong Min Kim, Woon Ki Cho, Jin Sook Song, Kyo Chul Lee, Ji-Ae Park, Myung Ae Bae, Jae Yong Choi, Minkyung Lee, Jin Chung, Chul Hoon Kim, Chul Hyoung Lyoo, Jee Hae Kang, Young Hoon Ryu |
| Weitere Verfasser: | College of Medicine, Dept. of Pharmacology, Jae Yong Choi, Jin Sook Song, Minkyung Lee, Woon-Ki Cho, Jin Chung, Chul Hyoung Lyoo, Chul Hoon Kim, Jiae Park, Kyo Chul Lee, Kyeong Min Kim, Jee Hae Kang, Myung Ae Bae, Young Hoon Ryu, Kim, Chul Hoon, Lyoo, Chul Hyoung, Ryu, Young Hoon, Choi, Jae Yong |
| Quelle: | Molecular Imaging and Biology. 18:267-273 |
| Verlagsinformationen: | Springer Science and Business Media LLC, 2015. |
| Publikationsjahr: | 2015 |
| Schlagwörter: | Male, Fluorine Radioisotopes, Pyridines, ATP Binding Cassette Transporter, Knockout, Quinolines/administration & dosage, P-glycoprotein, Piperazines, Rats, Sprague-Dawley, Mice, 03 medical and health sciences, [18F]Mefway, 0302 clinical medicine, Member 2/metabolism, Member 1/metabolism, ATP Binding Cassette Transporter, Subfamily G, Member 2, Animals, ATP Binding Cassette Transporter, Subfamily B, Member 1, Sub-Family G, Mice, Knockout, Piperazines/blood, Sub-Family B, Pyridines/pharmacokinetics, Brain, Piperazines/pharmacokinetics, Brain/diagnostic imaging, Fluorine Radioisotopes/pharmacokinetics, Brain/metabolism, Breast cancer resistance protein, Pyridines/blood, Rats, PET, Positron-Emission Tomography, Quinolines, ATP-Binding Cassette, Sprague-Dawley |
| Beschreibung: | The aim of this study was to determine whether the brain uptake of [(18)F]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents.[(18)F]Mefway was applied to rats pharmacologically inhibited with tariquidar (TQD) and to genetically disrupted mice.Pretreatment of TQD results in 160% higher hippocampal uptake compared with control rats. In genetically disrupted mice, a maximal brain uptake value of 3.2 SUV in the triple knockout mice (tKO, Mdr1a/b((-/-))Bcrp1((-/-))) was comparable to that of the double knockout mice (dKO, Mdr1a/b((-/-))) and 2-fold those of the wild-type and Bcrp1((-/-)) knockout mice. The differences of binding values were statistically insignificant between control and experimental groups. The brain-to-plasma ratios for tKO mice were also two to five times higher than those for other groups.[(18)F]Mefway is modulated by P-gp, and not by Bcrp in rodents. |
| Publikationsart: | Article |
| Dateibeschreibung: | 267~73 |
| Sprache: | English |
| ISSN: | 1860-2002 1536-1632 |
| DOI: | 10.1007/s11307-015-0883-z |
| Zugangs-URL: | https://pubmed.ncbi.nlm.nih.gov/26250653 http://europepmc.org/abstract/MED/26250653 https://ir.ymlib.yonsei.ac.kr/handle/22282913/146590 https://dspace.ewha.ac.kr/handle/2015.oak/217485 https://yonsei.pure.elsevier.com/en/publications/p-glycoprotein-not-bcrp-limits-the-brain-uptake-of-sup18sup-fmefw https://link.springer.com/article/10.1007/s11307-015-0883-z https://link.springer.com/article/10.1007/s11307-015-0883-z/fulltext.html |
| Rights: | Springer TDM CC BY NC ND |
| Dokumentencode: | edsair.doi.dedup.....8a603bfb1f5ce8da80b0b2b76f1db6e0 |
| Datenbank: | OpenAIRE |
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Nájsť tento článok vo Web of Science | Abstract: | The aim of this study was to determine whether the brain uptake of [(18)F]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents.[(18)F]Mefway was applied to rats pharmacologically inhibited with tariquidar (TQD) and to genetically disrupted mice.Pretreatment of TQD results in 160% higher hippocampal uptake compared with control rats. In genetically disrupted mice, a maximal brain uptake value of 3.2 SUV in the triple knockout mice (tKO, Mdr1a/b((-/-))Bcrp1((-/-))) was comparable to that of the double knockout mice (dKO, Mdr1a/b((-/-))) and 2-fold those of the wild-type and Bcrp1((-/-)) knockout mice. The differences of binding values were statistically insignificant between control and experimental groups. The brain-to-plasma ratios for tKO mice were also two to five times higher than those for other groups.[(18)F]Mefway is modulated by P-gp, and not by Bcrp in rodents. |
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| ISSN: | 18602002 15361632 |
| DOI: | 10.1007/s11307-015-0883-z |