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Compartmental Modeling of Iodine-123-Iodobenzofuran Binding to Dopamine D2 Receptors in Healthy Subjects

Departments of Psychiatry and Diagnostic Radiology, Yale University School of Medicine, New Haven
West Haven Veterans Affairs Medical Center, West Haven, Connecticut
Division of Nuclear Medicine, Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania

Correspondence: For correspondence or reprints contact: Marc Laruelle, MD, Department of Psychiatry, Yale School of Medicine, West Haven VA Medical Center/16A2, West Haven, CT 06516.

ABSTRACT

Iodine-123-labeled iodobenzofuran ([¹²³I]IBF) is a potent dopamine D2 antagonist that provides good visualization of D2 receptors in primates. Methods: The feasibility of measuring dopamine D2 binding potential with [¹²³I]IBF in humans was evaluated in eight healthy subjects. Following [¹²³I]IBF injection (6 mCi), scans were acquired every 10 min for 160 min with the brain-dedicated CERASPECT camera. Arterial activities were obtained at various intervals and corrected for the presence of metabolites by extraction followed by reverse-phase high-performance liquid chromatography. Results: Reconstructed images exhibited adequate basal ganglia-to-occipital ratios (from 1.96 ± 0.34 at 30 min to 3.54 ± 0.71 at 150 min, mean ± s.d.). Time activity curves demonstrated reversibility, with peak basal ganglia uptake at 50 ± 25 min. Regional time-activity curves were analyzed kinetic three-compartment modeling and graphic analysis. In all subjects, D2 binding potential values, as derived by both methods, were in excellent agreement (mean ± s.d. D2 binding potential = 129 ± 51). An empiric count ratio method that does not require measurement of arterial tracer concentrations was evaluated and found to be in reasonable agreement with the model-derived binding potential. Conclusion: Iodine 131-IBF is a suitable ligand for quantitative studies of D2 receptor density with SPECT in humans.

Key Words: SPECT • dopamine D2 receptors • iodine-123-IBF • kinetic analysis

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