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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Bibliographic Details
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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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.09.142