title: Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype.
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.
authors.affiliation: Department of Nuclear Medicine, Krankenhausstrasse 12, D-91054 Erlangen, Germany. carsten.hocke@nuklear.imed.uni-erlangen.de
authors.forename: Carsten
authors.initials: C
authors.lastname: Hocke
authors.forename: Olaf
authors.initials: O
authors.lastname: Prante
authors.forename: Stefan
authors.initials: S
authors.lastname: Löber
authors.forename: Harald
authors.initials: H
authors.lastname: Hübner
authors.forename: Peter
authors.initials: P
authors.lastname: Gmeiner
authors.forename: Torsten
authors.initials: T
authors.lastname: Kuwert
mesh_terms: D065127:Dopamine D2 Receptor Antagonists; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D007700:Kinetics; D008024:Ligands; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology
chemical_list: D065127:Dopamine D2 Receptor Antagonists; C467223:FAUC 365; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D008024:Ligands; D010879:Piperazines; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D013876:Thiophenes