PET radiotracers: crossing the blood-brain barrier and surviving metabolism.
PET radiotracers: crossing the blood-brain barrier and surviving metabolism.
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DOI：
10.1016/j.tips.2009.05.005
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发表时间：
2009-08
影响因子：
13.8
通讯作者：
Pike VW
中科院分区：
文献类型：
--
作者：
Pike VW
利用正电子发射断层扫描(PET)成像活体人脑蛋白质靶点的放射性示踪剂在临床研究和药物开发中越来越有用。这种放射性示踪剂必须满足许多标准，其中能够充分和可逆地进入大脑而不受麻烦的放射性代谢物污染是准确测量目标蛋白(例如，神经受体、转运体、酶或斑块)密度所必需的。候选放射性示踪剂可能会因为被动的大脑进入不良、外流转运蛋白对大脑的排斥或不良的代谢而失败。对这些问题进行了回顾。讨论了用于测量外排转运功能的新兴PET放射性示踪剂，以及改善放射性示踪剂代谢的新策略。随着对未来放射性示踪剂的分子特征影响的深入了解，放射性示踪剂的脑穿透、新陈代谢和外排转运敏感性最终将导致其更合理和更有效的设计，也将导致其更大的功效。
Radiotracers for imaging protein targets in living human brain with positron emission tomography (PET) are increasingly useful in clinical research and in drug development. Such radiotracers must fulfill many criteria, among which an ability to enter brain adequately and reversibly without contamination by troublesome radiometabolites is desirable for accurate measurement of the density of a target protein (e.g., neuroreceptor, transporter, enzyme or plaque). Candidate radiotracers may fail as a result of poor passive brain entry, rejection from brain by efflux transporters or undesirable metabolism. These issues are reviewed. Emerging PET radiotracers for measuring efflux transporter function, and new strategies for ameliorating radiotracer metabolism are discussed. A growing understanding of the molecular features affecting the brain penetration, metabolism and efflux transporter sensitivity of prospective radiotracers should ultimately lead to their more rational and efficient design, and also to their greater efficacy.
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影响因子：
6.3
作者：
Hinz, Rainer;Bhagwagar, Zubin;Grasby, Paul M.
通讯作者：
Grasby, Paul M.
影响因子：
7.3
作者：
Donohue SR;Krushinski JH;Pike VW;Chernet E;Phebus L;Chesterfield AK;Felder CC;Halldin C;Schaus JM
通讯作者：
Schaus JM
影响因子：
7.3
作者：
Briard E;Zoghbi SS;Siméon FG;Imaizumi M;Gourley JP;Shetty HU;Lu S;Fujita M;Innis RB;Pike VW
通讯作者：
Pike VW
DOI：
10.2967/jnumed.108.060186
发表时间：
2009-07
期刊：
Journal of nuclear medicine : official publication, Society of Nuclear Medicine
影响因子：
--
作者：
Fujimura Y;Zoghbi SS;Simèon FG;Taku A;Pike VW;Innis RB;Fujita M
通讯作者：
Fujita M
影响因子：
3.4
作者：
Farde, L;Ginovart, N;Halldin, C
通讯作者：
Halldin, C