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

doi:10.1016/j.bmcl.2009.07.103

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 journal › Article › peer-review

6 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 language	English
Pages (from-to)	5436-5439
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2009.07.103
Publication status	Published - 2009 Sept 15
Externally published	Yes

Keywords

NPY
Neuropeptide Y
PET ligand
Positron emission tomography

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2009.07.103

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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

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, vol. 19, no. 18, pp. 5436-5439. https://doi.org/10.1016/j.bmcl.2009.07.103

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doi = "10.1016/j.bmcl.2009.07.103",

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AU - Takahashi, Hirobumi

AU - Haga, Yuji

AU - Shibata, Takunobu

AU - Nonoshita, Katsumasa

AU - Sakamoto, Toshihiro

AU - Moriya, Minoru

AU - Ohe, Tomoyuki

AU - Chiba, Masato

AU - Mitobe, Yuko

AU - Kitazawa, Hidefumi

AU - Iwaasa, Hisashi

AU - Ishihara, Akane

AU - Ishii, Yasuyuki

AU - Kanatani, Akio

AU - Fukami, Takehiro

PY - 2009/9/15

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AB - 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.

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KW - Neuropeptide Y

KW - PET ligand

KW - Positron emission tomography

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

Abstract

Keywords

ASJC Scopus subject areas

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