Preprint Article Version 1 This version is not peer-reviewed

Synthesis and Initial In Vivo Evaluation of [11C]AZ683 – a Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R)

Version 1 : Received: 31 October 2018 / Approved: 2 November 2018 / Online: 2 November 2018 (02:55:47 CET)

A peer-reviewed article of this Preprint also exists.

Tanzey, S.S.; Shao, X.; Stauff, J.; Arteaga, J.; Sherman, P.; Scott, P.J.H.; Mossine, A.V. Synthesis and Initial In Vivo Evaluation of [11C]AZ683—A Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R). Pharmaceuticals 2018, 11, 136. Tanzey, S.S.; Shao, X.; Stauff, J.; Arteaga, J.; Sherman, P.; Scott, P.J.H.; Mossine, A.V. Synthesis and Initial In Vivo Evaluation of [11C]AZ683—A Novel PET Radiotracer for Colony Stimulating Factor 1 Receptor (CSF1R). Pharmaceuticals 2018, 11, 136.

Journal reference: Pharmaceuticals 2018, 11, 136
DOI: 10.3390/ph11040136

Abstract

Positron emission tomography (PET) imaging of Colony Stimulating Factor 1 Receptor (CSF1R) is a new strategy for quantifying both neuroinflammation and inflammation in the periphery since CSF1R is expressed on microglia. AZ683 has high affinity for CSF1R (Ki = 8 nM; IC50 = 6 nM) and >250-fold selectivity over 95 other kinases and, in this paper, we report the radiosynthesis of [11C]AZ683 and initial evaluation of its use in CSF1R PET. [11C]AZ683 was synthesized by 11C-methylation of the desmethyl precursor with [11C]MeOTf in 3.0% non-corrected activity yield (based upon [11C]MeOTf), >99% radiochemical purity and high specific activity. Preliminary PET imaging with [11C]AZ683 revealed no brain uptake in rodents and nonhuman primates suggesting that [11C]AZ683 is a poor candidate for imaging neuroinflammation, but that it could still be useful for peripheral imaging of inflammation.

Subject Areas

neuroinflammation; microglia; carbon-11; radiochemistry; positron emission tomography

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