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Synthesis and Initial Preclinical Evaluation of the P2X7 Receptor Antagonist [¹¹C]A-740003 as a Novel Tracer of Neuroinflammation

Synthesis and Initial Preclinical Evaluation of the P2X7 Receptor Antagonist [¹¹C]A-740003 as a Novel Tracer of Neuroinflammation

Bieneke Janssen, Danielle J Vugts, Uta Funke, Arnold Spaans, Robert C Schuit, Esther Kooijman, Marissa Rongen, Lars R Perk, Adriaan A Lammertsma, Albert D Windhorst

J Labelled Comp Radiopharm. 2014 Jun 30;57(8):509-16.

PMID: 24995673

Abstract:

Neuroinflammation, in particular activation of microglia, is thought to play an important role in the progression of neurodegenerative diseases. In activated microglia, the purinergic P2X7 receptor is upregulated. A-740003, a highly affine and selective P2X7 receptor antagonist, is a promising candidate for the development of a radiotracer for imaging of neuroinflammation by positron emission tomography. For this purpose, [(11)C]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 [(11)C]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 P2X7 receptor in healthy brain or to limited transport across the blood-brain barrier has yet to be elucidated.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP861393284	A-740003		861393-28-4	Price

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