494802-25-4Relevant academic research and scientific papers
Identification of positron emission tomography ligands for NPY Y5 receptors in the brain
Takahashi, Hirobumi,Haga, Yuji,Shibata, Takunobu,Nonoshita, Katsumasa,Sakamoto, Toshihiro,Moriya, Minoru,Ohe, Tomoyuki,Chiba, Masato,Mitobe, Yuko,Kitazawa, Hidefumi,Iwaasa, Hisashi,Ishihara, Akane,Ishii, Yasuyuki,Kanatani, Akio,Fukami, Takehiro
scheme or table, p. 5436 - 5439 (2010/05/19)
A series of trans-3-oxospiro[(aza)isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide derivatives were synthesized and profiled for NPY Y5 binding affinity, brain and CSF penetrability in rats, and susceptibility to human and mouse P-glycoprotein transporters in order to develop a PET ligand. Compound 12b exhibited an acceptable profile for a PET ligand, and [11C]12b was successfully utilized in clinical settings as a Y5 PET ligand.
