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 receptorsZhou, 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.
Research output: Contribution to journal › Article › Academic › peer-review
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.
|Number of pages||7|
|Journal||Journal of Medicinal Chemistry|
|Publication status||Published - 13-Nov-2014|
- POSITRON-EMISSION-TOMOGRAPHY, PARKINSONS-DISEASE, BASAL GANGLIA, LIGAND, RAT, ISTRADEFYLLINE, ANTAGONISTS, POTENT, BRAIN