title: Synthesis and evaluation of fluoro substituted  pyridinylcarboxamides and their phenylazo analogues  for potential dopamine D3 receptor PET imaging.
abstract: A series of fluoro substituted pyridinylcarboxamides and their phenylazo analogues with high affinity and selectivity for the dopamine D3 receptor was synthesized by the use of 6-fluoropyridine-3-carbonyl chloride (1) and fluorophenylazocarboxylic ester (2). Several of these compounds (9a-e and 10a-h) have been evaluated in vitro, among which 9b, 10a, 10c and 10d proved to have at least single-digit nanomolar affinity for D3. They also exhibit considerable selectivity over the other dopamine receptor subtypes and noteworthy selectivity over the structurally related serotonin receptor subtypes 5-HT(1A) and 5-HT₂, offering potential radiotracers for positron emission tomography.
authors.forename: Natascha
authors.initials: N
authors.lastname: Nebel
authors.forename: Simone
authors.initials: S
authors.lastname: Maschauer
authors.forename: Amelie L
authors.initials: AL
authors.lastname: Bartuschat
authors.forename: Stefanie K
authors.initials: SK
authors.lastname: Fehler
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
authors.forename: Markus R
authors.initials: MR
authors.lastname: Heinrich
authors.forename: Olaf
authors.initials: O
authors.lastname: Prante
authors.forename: Carsten
authors.initials: C
authors.lastname: Hocke
mesh_terms: D005462:Fluorine Radioisotopes; D006801:Humans; D015394:Molecular Structure; D049268:Positron-Emission Tomography / Q000379:methods*; D011869:Radioligand Assay; D050637:Receptors, Dopamine D3 / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D005462:Fluorine Radioisotopes; D050637:Receptors, Dopamine D3