1. [18F]Nifene test–retest reproducibility in first‐in‐human imaging of α4β2* nicotinic acetylcholine receptors
- Author
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Lao, Patrick J, Betthauser, Tobey J, Tudorascu, Dana L, Barnhart, Todd E, Hillmer, Ansel T, Stone, Charles K, Mukherjee, Jogeshwar, and Christian, Bradley T
- Subjects
Biomedical and Clinical Sciences ,Neurosciences ,Clinical Research ,Prevention ,Adult ,Aged ,Brain ,Brain Mapping ,Female ,Fluorine Radioisotopes ,Humans ,Kinetics ,Magnetic Resonance Imaging ,Male ,Middle Aged ,Positron-Emission Tomography ,Protein Binding ,Pyridines ,Pyrroles ,Radiopharmaceuticals ,Receptors ,Nicotinic ,Reproducibility of Results ,Young Adult ,alpha 4 beta 2 ,first-in-humans ,positron emission tomography ,α4β2 ,Cognitive Sciences ,Neurology & Neurosurgery - Abstract
The aim of this study was to examine the suitability of [18 F]nifene, a novel α4β2* nicotinic acetylcholine receptor (nAChR) radiotracer, for in vivo brain imaging in a first-in-human study. Eight healthy subjects (4 M,4 F;21-69,44 ± 21 yrs) underwent a [18 F]nifene positron emission tomography scan (200 ± 3.7 MBq), and seven underwent a second scan within 58 ± 31 days. Regional estimates of DVR were measured using the multilinear reference tissue model (MRTM2) with the corpus callosum as reference region. DVR reproducibility was evaluated with test-retest variability (TRV) and intraclass correlation coefficient (ICC). The DVR ranged from 1.3 to 2.5 across brain regions with a TRV of 0-7%, and did not demonstrate a systematic difference between test and retest. The ICCs ranged from 0.2 to 0.9. DVR estimates were stable after 40 min. The binding profile and tracer kinetics of [18 F]nifene make it a promising α4β2* nAChR radiotracer for scientific research in humans, with reliable DVR test-retest reproducibility.
- Published
- 2017