title: Repeated administration of D-amphetamine induces loss of [123I]FP-CIT binding to striatal dopamine transporters in rat brain: a validation study.
abstract: In recent years, several PET and SPECT studies have shown loss of striatal dopamine transporter (DAT) binding in amphetamine (AMPH) users. However, the use of DAT SPECT tracers to detect AMPH-induced changes in DAT binding has not been validated. We therefore examined if repeated administration of D-AMPH or methamphetamine (METH) may induce loss of binding to striatal DATs in rats by using an experimental biodistribution study design and a SPECT tracer for the DAT ([123I]FP-CIT).
  
  
  METHODS
  Groups of male rats (n = 10 per group) were treated with D-AMPH (10 mg/kg body weight), METH (10 mg/kg body weight), or saline, twice a day for 5 consecutive days. Five days later, [123I]FP-CIT was injected intravenously, and 2 h later, the rats were sacrificed and radioactivity was assayed.
  
  
  RESULTS
  In d-AMPH but not METH-treated rats, striatal [123I]FP-CIT uptake was significantly lower (approximately 17%) than in the control group.
  
  
  CONCLUSIONS
  These data show that [123I]FP-CIT can be used to detect AMPH-induced changes in DAT binding and may validate the use of DAT radiotracers to study AMPH-induced changes in striatal DAT binding in vivo.
authors.affiliation: Department of Nuclear Medicine, Academic Medical Center, 1105 AZ Amsterdam, The Netherlands. j.booij@amc.uva.nl
authors.forename: Jan
authors.initials: J
authors.lastname: Booij
authors.forename: Kora
authors.initials: K
authors.lastname: de Bruin
authors.forename: W Boudewijn
authors.initials: WB
authors.lastname: Gunning
mesh_terms: D000661:Amphetamine / Q000008:administration & dosage*; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D015259:Dopamine Agents / Q000008:administration & dosage*; D050483:Dopamine Plasma Membrane Transport Proteins / Q000378:metabolism*; D007457:Iodine Radioisotopes; D008297:Male; D008694:Methamphetamine / Q000008:administration & dosage; D051381:Rats; D017208:Rats, Wistar; D015899:Tomography, Emission-Computed, Single-Photon; D014326:Tropanes / Q000378:metabolism*
chemical_list: D015259:Dopamine Agents; D050483:Dopamine Plasma Membrane Transport Proteins; D007457:Iodine Radioisotopes; D014326:Tropanes; C087552:2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane; D008694:Methamphetamine; D000661:Amphetamine