Synthesis, biological evaluation and radiolabelling by 18F- fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET

S. B. Höfling; S. Maschauer; H. Hübner; P. Gmeiner; H. J. Wester; O. Prante; M. R. Heinrich

doi:10.1016/j.bmcl.2010.09.142

Synthesis, biological evaluation and radiolabelling by ¹⁸F- fluoroarylation of a dopamine D₃-selective ligand as prospective imaging probe for PET

S. B. Höfling
, S. Maschauer
, H. Hübner
, P. Gmeiner
, H. J. Wester
, O. Prante
, M. R. Heinrich

Chair of Pharmaceutical Radiochemistry

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

15 Scopus citations

Abstract

Radical ¹⁸F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D₃-selective ligand SH 317 ([ ¹⁸F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.

Original language	English
Pages (from-to)	6933-6937
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2010.09.142
State	Published - 1 Dec 2010

Keywords

18-Fluorine
Dopamine
Ligands
Positron emission tomography
Radiochemical labelling

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10.1016/j.bmcl.2010.09.142

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title = "Synthesis, biological evaluation and radiolabelling by 18F- fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET",

abstract = "Radical 18F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D3-selective ligand SH 317 ([ 18F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.",

keywords = "18-Fluorine, Dopamine, Ligands, Positron emission tomography, Radiochemical labelling",

author = "H{\"o}fling, \{S. B.\} and S. Maschauer and H. H{\"u}bner and P. Gmeiner and Wester, \{H. J.\} and O. Prante and Heinrich, \{M. R.\}",

note = "Funding Information: The authors would like to thank the Friedrich-Alexander-Universit{\"a}t Erlangen-N{\"u}rnberg (FAU) and the Deutsche Forschungsgemeinschaft (DFG) [DFG ( HE5413/3-1 ), DFG ( WE 2386/5-1 ), DFG ( PR 677/2-3 )] for generous financial support. ",

year = "2010",

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doi = "10.1016/j.bmcl.2010.09.142",

language = "English",

volume = "20",

pages = "6933--6937",

journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Synthesis, biological evaluation and radiolabelling by 18F- fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET

AU - Höfling, S. B.

AU - Maschauer, S.

AU - Hübner, H.

AU - Gmeiner, P.

AU - Wester, H. J.

AU - Prante, O.

AU - Heinrich, M. R.

N1 - Funding Information: The authors would like to thank the Friedrich-Alexander-Universität Erlangen-Nürnberg (FAU) and the Deutsche Forschungsgemeinschaft (DFG) [DFG ( HE5413/3-1 ), DFG ( WE 2386/5-1 ), DFG ( PR 677/2-3 )] for generous financial support.

PY - 2010/12/1

Y1 - 2010/12/1

N2 - Radical 18F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D3-selective ligand SH 317 ([ 18F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.

AB - Radical 18F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D3-selective ligand SH 317 ([ 18F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.

KW - 18-Fluorine

KW - Dopamine

KW - Ligands

KW - Positron emission tomography

KW - Radiochemical labelling

UR - https://www.scopus.com/pages/publications/78149279657

U2 - 10.1016/j.bmcl.2010.09.142

DO - 10.1016/j.bmcl.2010.09.142

M3 - Article

C2 - 21030255

AN - SCOPUS:78149279657

SN - 0960-894X

VL - 20

SP - 6933

EP - 6937

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

Synthesis, biological evaluation and radiolabelling by ¹⁸F- fluoroarylation of a dopamine D₃-selective ligand as prospective imaging probe for PET

Abstract

Keywords

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