PT  - JOURNAL ARTICLE
AU  - Zimmer, Luc
AU  - Hassoun, Waddad
AU  - Pain, Frederic
AU  - Bonnefoi, Frederic
AU  - Lanièce, Philippe
AU  - Mastrippolito, Roland
AU  - Pinot, Laurent
AU  - Pujol, Jean-François
AU  - Leviel, Vincent
TI  - SIC, an Intracerebral β<sup>+</sup>-Range–Sensitive Probe for Radiopharmacology Investigations in Small Laboratory Animals: Binding Studies with <sup>11</sup>C-Raclopride
DP  - 2002 Feb 01
TA  - Journal of Nuclear Medicine
PG  - 227--233
VI  - 43
IP  - 2
4099  - http://jnm.snmjournals.org/content/43/2/227.short
4100  - http://jnm.snmjournals.org/content/43/2/227.full
SO  - J Nucl Med2002 Feb 01; 43
AB  - 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.