期刊
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
卷 57, 期 8, 页码 509-516出版社
WILEY
DOI: 10.1002/jlcr.3206
关键词
radiolabelling; carbon-11; A-740003; P2X(7) receptor; neuroinflammation; positron emission tomography
资金
- European Union [HEALTH-F2-2011-278850]
Neuroinflammation, in particular activation of microglia, is thought to play an important role in the progression of neurodegenerative diseases. In activated microglia, the purinergic P2X(7) receptor is upregulated. A-740003, a highly affine and selective P2X(7) receptor antagonist, is a promising candidate for the development of a radiotracer for imaging of neuroinflammation by positron emission tomography. For this purpose, [C-11] A-740003 was synthesised and evaluated in vivo with respect to both tracer metabolism and biodistribution. In plasma, a moderate metabolic rate was seen. In healthy rat brain, only marginal uptake of [C-11] A-740003 was observed and, therefore, metabolites in brain could not be determined. Whether the minimal brain uptake is due to the low expression levels of the P2X(7) receptor in healthy brain or to limited transport across the blood-brain barrier has yet to be elucidated.
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