Booij J, Andringa G, Rijks L J, Vermeulen R J, De Bruin K, Boer G J, Janssen A G, Van Royen E A
Graduate School of Neurosciences, Department of Nuclear Medicine, University of Amsterdam, The Netherlands.
Synapse. 1997 Nov;27(3):183-90. doi: 10.1002/(SICI)1098-2396(199711)27:3<183::AID-SYN4>3.0.CO;2-9.
[123I]FP-CIT (N-omega-fluoropropyl-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane), a radioiodinated cocaine analogue, was evaluated as an agent for the in vivo labeling of dopamine (DA) transporters by biodistribution studies in rats and by single photon emission computed tomography (SPECT) studies in unilateral 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned monkeys. In rats, intravenous injection of [123I]FP-CIT resulted in high accumulation of radioactivity in the striatum. Less pronounced uptake was seen in brain areas with high densities of serotonergic uptake sites. While striatal uptake of radioactivity after injection of [123I]FP-CIT was displaced significantly by GBR12,909 but not by fluvoxamine, the opposite was observed in brain areas known to be rich of serotonin transporters. Monkeys which were unilaterally treated with neurotoxic doses of MPTP showed severe loss of striatal [123I]FP-CIT uptake at the side of treatment. The results of this study indicate that [123I]FP-CIT, although not being a selective radioligand, binds specifically to the striatal DA transporter in vivo and thus suggest that [123I]FP-CIT promises to be a suitable radioligand for SPECT imaging of DA transporters in humans.
[123I]FP-CIT（N-ω-氟丙基-2β-甲氧基羰基-3β-（4-碘苯基）-托烷），一种放射性碘化可卡因类似物，通过在大鼠身上进行的生物分布研究以及在单侧1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）损伤的猴子身上进行的单光子发射计算机断层扫描（SPECT）研究，被评估为一种用于体内标记多巴胺（DA）转运体的试剂。在大鼠中，静脉注射[123I]FP-CIT导致纹状体中放射性的高度积累。在血清素能摄取位点密度高的脑区，摄取不太明显。虽然注射[123I]FP-CIT后纹状体对放射性的摄取被GBR12,909显著取代，但未被氟伏沙明取代，而在已知富含血清素转运体的脑区观察到相反的情况。单侧接受神经毒性剂量MPTP治疗的猴子在治疗侧纹状体对[123I]FP-CIT的摄取严重丧失。这项研究的结果表明，[123I]FP-CIT虽然不是一种选择性放射性配体，但在体内能特异性结合纹状体DA转运体，因此表明[123I]FP-CIT有望成为一种适用于人类DA转运体SPECT成像的放射性配体。
