Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype

  • Bioorg Med Chem Lett. 2004 Aug 2;14(15):3963-6. doi: 10.1016/j.bmcl.2004.05.052.
Carsten Hocke  1 ,  Olaf Prante ,  Stefan Löber ,  Harald Hübner ,  Peter Gmeiner ,  Torsten Kuwert
Affiliations
  • 1. Department of Nuclear Medicine, Krankenhausstrasse 12, D-91054 Erlangen, Germany. [email protected]
PMID: 15225707 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.

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