title: In vivo PET quantification of the dopamine transporter in rat brain with [¹⁸F]LBT-999.
abstract: BACKGROUND
  We examined whether [(18)F]LBT-999 ((E)-N-(4-fluorobut-2-enyl)2β-carbomethoxy-3β-(4'-tolyl)nortropane) is an efficient positron emission tomography (PET) tracer for the quantification of the dopamine transporter (DAT) in the healthy rat brain.
  
  
  METHODS
  PET studies were performed using several experimental designs, i.e. test-retest, co-injection with different doses of unlabelled LBT, displacement with GBR12909 and pre-injection of amphetamine.
  
  
  RESULTS
  The uptake of [(18)F]LBT-999 confirmed its specific binding to the DAT. The non-displaceable uptake (BP(ND)) in the striatum, between 5.37 and 4.39, was highly reproducible and reliable, and was decreased by 90% by acute injection of GBR12909. In the substantia nigra/ventral tegmental area (SN/VTA), the variability was higher and the reliability was lower. Pre-injection of amphetamine induced decrease of [(18)F]LBT-999 BP(ND) of 50% in the striatum.
  
  
  CONCLUSIONS
  [(18)F]LBT-999 allows the quantification of the DAT in living rat brain with high reproducibility, sensitivity and specificity. It could be used to quantify the DAT in rodent models, thereby allowing to study neurodegenerative and neuropsychiatric diseases.
authors.affiliation: Inserm, U930, Tours, France; Université François-Rabelais de Tours, UMR-U930, Tours, France.
authors.forename: Sophie
authors.initials: S
authors.lastname: Sérrière
authors.forename: Clovis
authors.initials: C
authors.lastname: Tauber
authors.forename: Johnny
authors.initials: J
authors.lastname: Vercouillie
authors.forename: Denis
authors.initials: D
authors.lastname: Guilloteau
authors.forename: Jean-Bernard
authors.initials: JB
authors.lastname: Deloye
authors.forename: Lucette
authors.initials: L
authors.lastname: Garreau
authors.forename: Laurent
authors.initials: L
authors.lastname: Galineau
authors.forename: Sylvie
authors.initials: S
authors.lastname: Chalon
mesh_terms: D000661:Amphetamine / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000187:drug effects / Q000378:metabolism*; D003042:Cocaine / Q000031:analogs & derivatives*; D050483:Dopamine Plasma Membrane Transport Proteins / Q000378:metabolism*; D005462:Fluorine Radioisotopes; D007700:Kinetics; D008297:Male; D049268:Positron-Emission Tomography; D051381:Rats; D017208:Rats, Wistar; D015203:Reproducibility of Results
chemical_list: C508666:8-((E)-4-fluoro-but-2-enyl)-3beta-p-tolyl-8-aza-bicyclo(3.2.1)octane-2beta-carboxylic acid methyl ester; D050483:Dopamine Plasma Membrane Transport Proteins; D005462:Fluorine Radioisotopes; D000661:Amphetamine; D003042:Cocaine
keywords: PET; Quantification model; Small animal imaging; Tropane derivative