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Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype
Carsten Hocke1, Olaf Prante, Stefan Löber
1Department of Nuclear Medicine, Krankenhausstrasse 12, D-91054 Erlangen, Germany. carsten.hocke@nuklear.imed.uni-erlangen.de
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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Separation of the aromatic...