Abstract.
Serotonin-1A (5-HT1A) receptors are implicated in neurochemical mechanisms underlying anxiety and depression and their treatment. Animal studies have suggested that 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p-[18F]fluorobenzamido] ethyl] piperazine (p-MPPF) may be a suitable positron emission tomography (PET) tracer of 5-HT1A receptors. To test p-MPPF in humans, we performed 60-min dynamic PET scans in 13 healthy volunteers after single bolus injection. Metabolite quantification revealed a fast decrease in tracer plasma concentration, such that at 5 min post injection about 25% of the total radioactivity in plasma corresponded to p-MPPF. Radioactivity concentration was highest in hippocampus, intermediate in neocortex and lowest in basal ganglia and cerebellum. The interactions between p-MPPF and 5-HT1A receptors were described using linear compartmental models with plasma input and reference tissue approaches. The two quantification methods provided similar results which are in agreement with previous reports on 5-HT1A receptor brain distribution. In conclusion, our results show that p-MPPF is a suitable PET radioligand for 5-HT1A receptor human studies.
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Received 15 July and in revised form 30 September 2001
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Sanabria-Bohórquez, S.M., Biver, F., Damhaut, P. et al. Quantification of 5-HT1A receptors in human brain using p-MPPF kinetic modelling and PET. Eur J Nucl Med 29, 76–81 (2002). https://doi.org/10.1007/s00259-001-0684-2
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DOI: https://doi.org/10.1007/s00259-001-0684-2