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

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6933-7. doi: 10.1016/j.bmcl.2010.09.142. Epub 2010 Oct 26.

Authors

S B Höfling¹, S Maschauer, H Hübner, P Gmeiner, H-J Wester, O Prante, M R Heinrich

Affiliation

¹ Department für Chemie und Pharmazie, Pharmazeutische Chemie, Friedrich-Alexander-Universität Erlangen-Nürnberg, Erlangen, Germany.

PMID: 21030255
DOI: 10.1016/j.bmcl.2010.09.142

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Brain / metabolism
Dopamine
Fluorine Radioisotopes*
Isotope Labeling
Ligands
Positron-Emission Tomography*
Radiopharmaceuticals / chemical synthesis*
Radiopharmaceuticals / pharmacokinetics
Rats
Receptors, Dopamine D3 / chemistry*

Substances

Fluorine Radioisotopes
Ligands
Radiopharmaceuticals
Receptors, Dopamine D3
Dopamine