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SIC, an Intracerebral ß⁺-Range–Sensitive Probe for Radiopharmacology Investigations in Small Laboratory Animals: Binding Studies with ¹¹C-Raclopride

¹ Centre d’Exploration et de Recherche Médicales par Émission de Positons, Biomedical Cyclotron, Lyon, France
² CNRS ERS2019, Villeurbanne, France
³ Institut de Physique Nucléaire, Orsay, France

Our aim was to show the ability of a recently developed ß⁺-range–sensitive intracerebral probe (SIC) to measure, in vivo, the binding of radioligands in small animals. Methods: The potential of the device for pharmacokinetic studies was evaluated by measurement of the dynamic striatal binding of ¹¹C-raclopride, a well-documented D₂ dopaminergic receptor ligand, in rat brain after intravenous injection of the labeled compound. The effects of preinjection of the unlabeled ligand (raclopride, 2 mg/kg intravenously) and of increasing the synaptic dopamine level (amphetamine treatment, 1 mg/kg intravenously) or of depleting synaptic dopamine (reserpine pretreatment, 5 mg/kg intraperitoneally) on in vivo ¹¹C-raclopride binding were monitored by SIC. Results: The radioactivity curves measured as a function of time were reproducible and consistent with previous studies using PET imaging (ratio of striatum to cerebellum, 2.6 ± 0.3 after 20 min). Further studies showed significant displacement of ¹¹C-raclopride by its stable analog. Finally, the device proved its capacity to accurately detect changes in ¹¹C-raclopride binding after a sudden (amphetamine) or a gradual (reserpine) modulation of endogenous dopamine levels. Conclusion: These results show that the new device can monitor binding of PET ligands in anesthetized rodents in vivo, with high temporal resolution.

Key Words: ß⁺-range–sensitive probe • PET • dopamine D₂ receptor • rat • ¹¹C-raclopride • competitive binding

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