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

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

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.

Original language	English
Pages (from-to)	1773-1777
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2005.02.049
State	Published - 1 Apr 2005
Externally published	Yes

Keywords

4-Anilidopiperidines
Fluorine-18
Opioid receptor imaging
Positron emission tomography
Sufentanil

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10.1016/j.bmcl.2005.02.049

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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",

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

language = "English",

volume = "15",

pages = "1773--1777",

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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AN - SCOPUS:15044364686

SN - 0960-894X

VL - 15

SP - 1773

EP - 1777

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

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

Abstract

Keywords

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