Abstract
A novel positron emission tomography (PET) radiotracer, 6-[ 18F]fluoro-3-(2( S)-azetidinylmethoxy)pyridine (6-[ 18F]fluoro-A-85380, 6-[ 18F]FA) was synthesized by a no-carrier-added fluorination. In vitro 6-[ 18F]FA bound to nicotinic acetylcholine receptors (nAChRs), with very high affinity (K d 28 pM). In PET studies, 6-[ 18F]FA specifically labeled central nAChRs in the brain of the Rhesus monkey and demonstrated highest levels of accumulation of radioactivity in brain regions enriched with the α 4β 2 subtype of nAChR. 6-[ 18F]FA exhibited a target-to-non-target ratio (estimated as radioactivity in the thalamus to that in the cerebellum) of binding in primate brain similar to that previously determined for a labeled analog of epibatidine, [ 18F]FPH. In contrast to [ 18F]FPH, the novel tracer is expected to exhibit substantially less toxicity. Thus, the novel radioligand, 6-[ 18F]FA, appears to be a suitable candidate for imaging nAChRs in human brain. Published by Elsevier Science Inc.
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