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

Radical (18)F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D(3)-selective ligand SH 317 ([(18)F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.

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Published in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6933-6937
Main Authors:	HÖFLING, S. B, MASCHAUER, S, HÜBNER, H, GMEINER, P, WESTER, H.-J, PRANTE, O, HEINRICH, M. R
Format:	Article
Language:	English
Subjects:	Animals Biological and medical sciences Brain - metabolism Catecholaminergic system Contrast media. Radiopharmaceuticals Dopamine Fluorine Radioisotopes Isotope Labeling Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Positron-Emission Tomography Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics Rats Receptors, Dopamine D3 - chemistry
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container_title	Bioorganic & medicinal chemistry letters
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creator	HÖFLING, S. B MASCHAUER, S HÜBNER, H GMEINER, P WESTER, H.-J PRANTE, O HEINRICH, M. R
description	Radical (18)F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D(3)-selective ligand SH 317 ([(18)F]8). SH 317 has been evaluated as a new PET ligand candidate by in vivo experiments.
doi_str_mv	10.1016/j.bmcl.2010.09.142
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subjects	Animals Biological and medical sciences Brain - metabolism Catecholaminergic system Contrast media. Radiopharmaceuticals Dopamine Fluorine Radioisotopes Isotope Labeling Ligands Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Positron-Emission Tomography Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics Rats Receptors, Dopamine D3 - chemistry
title	Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET
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