@article {Kim1768, author = {Su Jin Kim and Jong Jin Lee and Hyun Soo Park and Byung Seok Moon and Ji Sun Kim and Byung Chul Lee and Yu Kyeong Kim and Sang Eun Kim}, title = {Kinetic brain analysis and whole-body imaging of 18F-haloperidol in healthy human subjects}, volume = {51}, number = {supplement 2}, pages = {1768--1768}, year = {2010}, publisher = {Society of Nuclear Medicine}, abstract = {1768 Objectives Haloperidol is one of the widely used antipsychotic drugs. We examined the regional distribution and clearance of haloperidol in the human brain using 18F-haloperidol to establish a kinetic modeling analysis method for the quantitative PET studies. Also we have used whole-body PET/CT to characterize the biodistribution in healthy human subject. Methods Dynamic 18F-haloperidol brain PET scans were acquired for 6 hour in 3 subjects. Arterial blood activities were obtained. We investigated kinetic models of haloperidol in striatal and extra-striatal region. Two-tissue compartment models with reversible (2T5P) and irreversible phosphorylation (k4=0, 2T4P), and the single-tissue compartment model (1T3P) were examined. Akaike Information Criterion (AIC) and F statistics were used to select the best model for the data set. Whole-body dynamic scans from the midfemoral position to the head were obtained over 24 hour. Results 18F-haloperidol shows high retention not only in doparminergic regions but also in cortical and cerebellum region. Peak uptake occurred at 50-60min after injection. The percent of 18F-haloperidol in plasma decreased with time, with 81\%, 55\%, 42\% and 33\% remaining at 1, 5, 15 and 30 min, respectively. For brain dynamic PET data, the 1T3P model best described tissue time-activity curves for doparminergic and nondopaminergic regions. In whole-body PET, brain, heart, kidney, liver, lung and small intestine showed significant tracer accumulation. Haloperidol decreased gradually in the lung and kidney, but increased in liver until 24 hour. Brain and heart decreased only 20-30\% at 24 hour. Conclusions The kinetic modeling analysis with 1T3P compartment model provided reliable binding parameters in 18F-haloperidol PET. The whole-body biodistribution would be useful for understanding the metabolic pathway and toxicity of 18F-haloperidol PET}, issn = {0161-5505}, URL = {https://jnm.snmjournals.org/content/51/supplement_2/1768}, eprint = {https://jnm.snmjournals.org/content}, journal = {Journal of Nuclear Medicine} }