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

Journal of Nuclear Medicine

Frederic Pain¹  Laurent Pinot¹  Roland Mastrippolito¹  Frederic Bonnefoi¹  Philippe Lanièce¹  Waddad Hassoun¹  Jean-François Pujol¹  Luc Zimmer¹  Vincent Leviel¹ 

关键词: β⁺-range–sensitive probe;    PET;    dopamine D₂ receptor;    rat;    ¹¹C-raclopride;    competitive binding;   

DOI  :  

学科分类：医学（综合）

来源: Society of Nuclear Medicine

【 摘 要 】

Our aim was to show the ability of a recently developed β+-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.

【 授权许可】

Unknown