P-Glycoprotein, not BCRP, Limits the Brain Uptake of [18F]Mefway in Rodent Brain

被引：4

作者：

Choi, Jae Yong ^{[1
]}

Song, Jin Sook ^{[2
]}

Lee, Minkyung ^{[3
]}

Cho, Woon-Ki ^{[2
]}

Chung, Jin ^{[4
,5
]}

Lyoo, Chul Hyoung ^{[6
]}

Kim, Chul Hoon ^{[7
,8
]}

Park, Jiae ^{[9
]}

Lee, Kyo Chul ^{[9
]}

Kim, Kyeong Min ^{[9
]}

Kang, Jee Hae ^{[10
]}

Bae, Myung Ae ^{[2
]}

Ryu, Young Hoon ^{[1
]}

机构：

[1] Yonsei Univ, Coll Med, Gangnam Severance Hosp, Dept Nucl Med, 712 Eonjuro, Seoul 135720, South Korea

[2] Korea Res Inst Chem Technol, Drug Discovery Div, Drug Discovery Platform Technol Grp, Daejeon, South Korea

[3] Inha Univ, Inha Univ Hosp, Coll Med, Dept Nucl Med, Inchon, South Korea

[4] Ewha Womans Univ, Sch Med, Dept Radiol, Seoul, South Korea

[5] Yonsei Univ, Coll Med, Dept Radiol, Seoul 120749, South Korea

[6] Yonsei Univ, Coll Med, Gangnam Severance Hosp, Dept Neurol, Seoul 120749, South Korea

[7] Yonsei Univ, Coll Med, Dept Pharmacol, Seoul 120749, South Korea

[8] Yonsei Univ, Coll Med, Brain Korea PLUS Project Med Sci 21, Seoul 120749, South Korea

[9] Korea Inst Radiol & Med Sci, Mol Imaging Res Ctr, Seoul, South Korea

[10] Swarthmore Coll, Dept Chem & Biochem, 500 Coll Ave, Swarthmore, PA 19081 USA

来源：

MOLECULAR IMAGING AND BIOLOGY | 2016年 / 18卷 / 02期

基金：

新加坡国家研究基金会;

关键词：

F-18] Mefway; P-glycoprotein; Breast cancer resistance protein; PET; POSITRON-EMISSION-TOMOGRAPHY; SEROTONIN 5-HT1A RECEPTORS; MULTIDRUG-RESISTANCE; BLOOD; PET; BARRIER; RADIOLIGAND; BINDING; MICROPET; TRANSPORTERS;

D O I：

10.1007/s11307-015-0883-z

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

Purpose The aim of this study was to determine whether the brain uptake of [F-18]Mefway is influenced by the action of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp) in rodents. Procedures: [F-18]Mefway was applied to rats pharmacologically inhibited with tariquidar (TQD) and to genetically disrupted mice. Results: 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. Conclusions: [F-18]Mefway is modulated by P-gp, and not by Bcrp in rodents.

引用

页码：267 / 273

页数：7

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