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Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors

Zhou, X., Khanapur, S., Huizing, A. P., Zijlma, R., Schepers, M., Dierckx, R. A. J. O., van Waarde, A., de Vries, E. & Elsinga, P., 13-Nov-2014, In : Journal of Medicinal Chemistry. 57, 21, p. 9204-9210 7 p.

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  • Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1

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DOI

2-(2-Furanyl)-7-[2-[4-[4-(2-[C-11]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine [(11)C]-3 ([C-11]Preladenant) was developed for mapping cerebral adenosine A2A receptors (A2ARs) with PET. The tracer was synthesized in high specific activity and purity. Tissue distribution was studied by PET imaging, ex vivo biodistribution (BD), and in vitro autoradiography (ARG) experiments. Regional brain uptake of [C-11]-3 was consistent with known A(2A)Rs distribution, with highest uptake in striatum. The results indicate that [C-11]-3 has favorable brain kinetics and exhibits suitable characteristics as an A(2A)R PET tracer.

Original languageEnglish
Pages (from-to)9204-9210
Number of pages7
JournalJournal of Medicinal Chemistry
Volume57
Issue number21
Publication statusPublished - 13-Nov-2014

    Keywords

  • POSITRON-EMISSION-TOMOGRAPHY, PARKINSONS-DISEASE, BASAL GANGLIA, LIGAND, RAT, ISTRADEFYLLINE, ANTAGONISTS, POTENT, BRAIN

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