Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents

Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T (2005)

Publication Type: Journal article

Publication year: 2005

Journal

Publisher: Elsevier

Book Volume: 15

Pages Range: 4819-4823

DOI: 10.1016/j.bmcl.2005.07.037

Abstract

A series of fluoro substituted aryl carboxamides was synthesized revealing high affinity for the dopamine D3 receptor. In contrast to 2-methoxy substitution, a 2,3-dichloro substitution pattern at the phenylpiperazine moiety induces a 10-fold increase of D3 affinity which is expressed by Ki values of 0.53, 1.1, and 9.0 nM for 8b, 8d, and 8f. Applying aromatic ¹⁸F-for-Br(Cl) substitution, high radiochemical yields between 76-82% were obtained for [¹⁸F]8c-f. The most promising ligand, [ ¹⁸F]8d, was used as imaging agent of the D3 receptor in vitro. However, due to the lack of specific binding, further studies should aim at the development of radioligands with improved D3 receptor selectivity. © 2005 Elsevier Ltd. All rights reserved.

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How to cite

APA:

Prante, O., Löber, S., Hübner, H., Gmeiner, P., & Kuwert, T. (2005). Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents. Bioorganic & Medicinal Chemistry Letters, 15, 4819-4823. https://doi.org/10.1016/j.bmcl.2005.07.037

MLA:

Prante, Olaf, et al. "Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents." Bioorganic & Medicinal Chemistry Letters 15 (2005): 4819-4823.

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