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

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

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

Affiliation

Höfling SB; Department für Chemie und Pharmazie, Pharmazeutische Chemie, Friedrich-Alexander-Universität Erlangen-Nürnberg, Erlangen, Germany.

Bioorg Med Chem Lett ; 20(23): 6933-7, 2010 Dec 01.

Article in En | MEDLINE | ID: mdl-21030255

ABSTRACT

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.

Subject(s)

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

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Fluorine Radioisotopes / Radiopharmaceuticals / Positron-Emission Tomography / Receptors, Dopamine D3 Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2010 Type: Article Affiliation country: Germany

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