TY - JOUR T1 - Nicotinic acetylcholine receptor binding of [F-18]Nifene in the rhesus monkey JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 1183 LP - 1183 VL - 52 IS - supplement 1 AU - Ansel Hillmer AU - Dustin Wooten AU - Jeff Moirano AU - Jonathan Engle AU - Todd Barnhart AU - Robert Nickles AU - Dhanabalan Murali AU - Mary Schneider AU - Jogeshwar Mukherjee AU - Bradley Christian Y1 - 2011/05/01 UR - http://jnm.snmjournals.org/content/52/supplement_1/1183.abstract N2 - 1183 Objectives The agonist [F-18]Nifene (NIF) is a PET radioligand developed to image α4β2 nicotinic acetylcholine receptors (nAChR). This work aims to assess the in vivo imaging characteristics of NIF in rhesus monkeys for the development of PET experiments for nACHR assay. Methods Dynamic PET imaging experiments with NIF were acquired in 4 anesthetized macaca mulatta (rhesus) monkeys using a microPET P4 scanner. Acquisition was initiated with a bolus injection of 3 ± 0.5 mCi of NIF. An injection of (-)-nicotine (0.03 mg/kg, i.v.) was given 45-60 minutes post injection to measure the displacement of NIF receptor binding. A second injection of NIF was given after 30 minutes to measure NIF nondisplaceable uptake. Time activity curves were extracted in the high uptake areas of the thalamus and lateral geniculate region (LG), and the cerebellum for the measurement of target-to-cerebellum ratios (T/C). Results High specific binding was observed in the thalamus and LG. T/C reached a plateau at 25-30 minutes post injection with values of 3.0, 2.4, 3.3, 3.1 for the thalamus, and 2.5, 2.2, 3.0, 2.6 for the LG. Elevated binding of NIF was observed in the subiculum, insular cortex, temporal cortex, and cingulate gyrus. The (-)-nicotine completely displaced NIF, with uptake falling to background levels within 15 minutes post-drug. Negligible displacement of NIF was observed in the cerebellum, suggesting potential as a reference region. Logan DVR estimates using the cerebellum yielded values of 2.8, 2.7, 3.0, 2.8 in the thalamus, and 2.3, 2.3, 2.3, 2.4 in the LG. The post-nicotine injection displayed uniform nondisplaceable uptake of NIF throughout gray and white brain matter. Conclusions In the rhesus monkey, [F-18]Nifene exhibits high specific binding and rapid equilibration in the thalamus and LG. Future work is ongoing to evaluate the behavior of NIF in arterial plasma. These results suggest NIF shows great promise for assessing nACHR binding. Research Support CA143188, AA01770 ER -