Identification of positron emission tomography ligands for NPY Y5 receptors in the brain

Hirobumi Takahashi, Yuji Haga, Takunobu Shibata, Katsumasa Nonoshita, Toshihiro Sakamoto, Minoru Moriya, Tomoyuki Ohe, Masato Chiba, Yuko Mitobe, Hidefumi Kitazawa, Hisashi Iwaasa, Akane Ishihara, Yasuyuki Ishii, Akio Kanatani, Takehiro Fukami

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)5436-5439
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number18
DOIs
Publication statusPublished - 2009 Sep 15
Externally publishedYes

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Keywords

  • Neuropeptide Y
  • NPY
  • PET ligand
  • Positron emission tomography

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

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., & Fukami, T. (2009). Identification of positron emission tomography ligands for NPY Y5 receptors in the brain. Bioorganic and Medicinal Chemistry Letters, 19(18), 5436-5439. https://doi.org/10.1016/j.bmcl.2009.07.103