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

研究成果: Article

4 引用 (Scopus)

抜粋

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.

元の言語English
ページ(範囲)5436-5439
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
19
発行部数18
DOI
出版物ステータスPublished - 2009 9 15
外部発表Yes

    フィンガープリント

ASJC Scopus subject areas

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

これを引用

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