18F-Labeled sufentanil for PET-imaging of μ-opioid receptors

Gjermund Henriksen; Stefan Platzer; Andrea Hauser; Frode Willoch; Achim Berthele; Markus Schwaiger; Hans Jürgen Wester

doi:10.1016/j.bmcl.2005.02.049

¹⁸F-Labeled sufentanil for PET-imaging of μ-opioid receptors

Gjermund Henriksen, Stefan Platzer, Andrea Hauser, Frode Willoch, Achim Berthele, Markus Schwaiger, Hans Jürgen Wester

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11 Zitate (Scopus)

Abstract

The synthesis of an ¹⁸F-labeled sufentanil analogue with apparent high μ-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N- phenyl-2-(±)-[¹⁸F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the μ-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in μ-opioid receptor mapping and quantitation with positron emission tomography.

Originalsprache	Englisch
Seiten (von - bis)	1773-1777
Seitenumfang	5
Fachzeitschrift	Bioorganic and Medicinal Chemistry Letters
Jahrgang	15
Ausgabenummer	7
DOIs	https://doi.org/10.1016/j.bmcl.2005.02.049
Publikationsstatus	Veröffentlicht - 1 Apr. 2005

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10.1016/j.bmcl.2005.02.049

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@article{6d80ad90de34437484e6442e1768a518,

title = "18F-Labeled sufentanil for PET-imaging of μ-opioid receptors",

abstract = "The synthesis of an 18F-labeled sufentanil analogue with apparent high μ-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N- phenyl-2-(±)-[18F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the μ-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in μ-opioid receptor mapping and quantitation with positron emission tomography.",

keywords = "4-Anilidopiperidines, Fluorine-18, Opioid receptor imaging, Positron emission tomography, Sufentanil",

author = "Gjermund Henriksen and Stefan Platzer and Andrea Hauser and Frode Willoch and Achim Berthele and Markus Schwaiger and Wester, {Hans J{\"u}rgen}",

note = "Funding Information: Financial support was received from the Norwegian Research Council, Project no. 151445/432 and from SFB 391 of the Deutsche Forschungsgemeinschaft.",

year = "2005",

month = apr,

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doi = "10.1016/j.bmcl.2005.02.049",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - 18F-Labeled sufentanil for PET-imaging of μ-opioid receptors

AU - Henriksen, Gjermund

AU - Platzer, Stefan

AU - Hauser, Andrea

AU - Willoch, Frode

AU - Berthele, Achim

AU - Schwaiger, Markus

AU - Wester, Hans Jürgen

N1 - Funding Information: Financial support was received from the Norwegian Research Council, Project no. 151445/432 and from SFB 391 of the Deutsche Forschungsgemeinschaft.

PY - 2005/4/1

Y1 - 2005/4/1

N2 - The synthesis of an 18F-labeled sufentanil analogue with apparent high μ-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N- phenyl-2-(±)-[18F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the μ-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in μ-opioid receptor mapping and quantitation with positron emission tomography.

AB - The synthesis of an 18F-labeled sufentanil analogue with apparent high μ-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N- phenyl-2-(±)-[18F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the μ-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in μ-opioid receptor mapping and quantitation with positron emission tomography.

KW - 4-Anilidopiperidines

KW - Fluorine-18

KW - Opioid receptor imaging

KW - Positron emission tomography

KW - Sufentanil

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DO - 10.1016/j.bmcl.2005.02.049

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SN - 0960-894X

VL - 15

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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