title: 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.
abstract: 2-(2-Furanyl)-7-[2-[4-[4-(2-[(11)C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine [(11)C]-3 ([(11)C]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 [(11)C]-3 was consistent with known A2ARs distribution, with highest uptake in striatum. The results indicate that [(11)C]-3 has favorable brain kinetics and exhibits suitable characteristics as an A2AR PET tracer.
authors.affiliation: Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Center Groningen , Hanzeplein 1, 9713GZ Groningen, The Netherlands.
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Zhou
authors.forename: Shivashankar
authors.initials: S
authors.lastname: Khanapur
authors.forename: Anja P
authors.initials: AP
authors.lastname: Huizing
authors.forename: Rolf
authors.initials: R
authors.lastname: Zijlma
authors.forename: Marianne
authors.initials: M
authors.lastname: Schepers
authors.forename: Rudi A J O
authors.initials: RA
authors.lastname: Dierckx
authors.forename: Aren
authors.initials: A
authors.lastname: van Waarde
authors.forename: Erik F J
authors.initials: EF
authors.lastname: de Vries
authors.forename: Philip H
authors.initials: PH
authors.lastname: Elsinga
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D007553:Isotope Labeling; D008297:Male; D049268:Positron-Emission Tomography / Q000379:methods; D011743:Pyrimidines / Q000097:blood / Q000138:chemical synthesis; D017208:Rats, Wistar; D043705:Receptor, Adenosine A2A / Q000378:metabolism; D014018:Tissue Distribution; D014230:Triazoles / Q000097:blood / Q000138:chemical synthesis
chemical_list: D011743:Pyrimidines; D043705:Receptor, Adenosine A2A; D014230:Triazoles; C539997:2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7H-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine