Identification of positron emission tomography ligands for NPY...

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Identification of positron emission tomography ligands for NPY Y5 receptors in the brain.
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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 [(11)C]12b was successfully utilized in clinical settings as a Y5 PET ligand.
Takahashi H, Haga Y, Shibata T, Nonoshita K, Sakamoto T, Moriya M, Ohe T, Chiba M, Mitobe Y, Kitazawa H, Iwaasa H, Ishihara A, Ishii Y, Kanatani A, and Fukami T
Bioorganic & medicinal chemistry letters 19(18):5436-9, 2009 Sep 15 - Who cited this? | PubMed ID: 19679469 | Fulltext
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