Synthesis and Radioiodination of Selective Ligands for the Dopamine D3 Receptor Subtype

Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T (2004)

Publication Type: Journal article

Publication year: 2004

Journal

Bioorganic & Medicinal Chemistry Letters Elsevier

Publisher: Elsevier

Book Volume: 14

Pages Range: 3963-3966

DOI: 10.1016/j.bmcl.2004.05.052

Abstract

Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding data showed a 15-560-fold selectivity for the dopamine D3 over D2. A 2,3-dichloro substitution pattern on the phenylpiperazine moiety led to the highest subtype selectivity, whereas the 2-methoxy substituted compounds showed superior D3 affinity. Suitable precursors were radioiodinated with high radiochemical yields (53-85%) leading to potential imaging agents for the D3 receptor by SPET. © 2004 Elsevier Ltd. All rights reserved.

Authors with CRIS profile

Olaf Prante Professur für Molekulare Bildgebung und Radiochemie Stefan Löber Lehrstuhl für Pharmazeutische Chemie Harald Hübner Lehrstuhl für Pharmazeutische Chemie Peter Gmeiner Lehrstuhl für Pharmazeutische Chemie Torsten Kuwert Lehrstuhl für Klinische Nuklearmedizin

How to cite

APA:

Prante, O., Löber, S., Hübner, H., Gmeiner, P., & Kuwert, T. (2004). Synthesis and Radioiodination of Selective Ligands for the Dopamine D3 Receptor Subtype. Bioorganic & Medicinal Chemistry Letters, 14, 3963-3966. https://doi.org/10.1016/j.bmcl.2004.05.052

MLA:

Prante, Olaf, et al. "Synthesis and Radioiodination of Selective Ligands for the Dopamine D3 Receptor Subtype." Bioorganic & Medicinal Chemistry Letters 14 (2004): 3963-3966.

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