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- W10383471 abstract "1217 Objectives: Brain serotonin 1A receptors (5-HT1A) exist in high- and low-affinity states. It is known that agonists bind preferentially to the high-affinity state of the receptor and therefore could provide a measure of the functional 5-HT1A receptors. Since all available PET 5-HT1A radiopharmaceuticals are antagonists, it is of great interest to develop a fluorine-18 labelled agonist. Methods: F15599 (3-chloro-4-fluorophenyl-(4-fluoro-4{[(5-methyl-pyrimidin-2-ylmethyl)-ammino]-methyl}-piperidin-1-yl)-methadone) is a novel ligand with high affinity and selectivity for 5-HT1A receptors (J Med Chem 2007, 50, 5024-5033). Its nitro-precursor was synthesized and radiolabelled via a fluoronucleophilic substitution. Radiopharmacological evaluations included in vitro and ex vivo autoradiographies in rat brain and PETscans on rats and cats. All results were compared with simultaneous studies using [18F]MPPF, a validated 5-HT1A radiopharmaceutical. Results: The chemical and radiochemical purities of [18F]F15599 were > 99%. The [18F]F15599 in vitro binding was consistent with the 5-HT1A receptors distribution (hippocampus, dorsal raphe nucleus and notably cortical areas). The ex vivo and in vivo studies revealed that the radiotracer readily entered the brain, but displayed a lack of specificity for 5-HT1A receptor rich regions. It is probably explained by the formation of radioactive metabolites. Conclusions: [18F]F15599 has suitable characteristics for probing in vitro the high-affinity states of the 5-HT1A receptors. However further chemical modifications are necessary for the in vivo use of this agonist." @default.
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- W10383471 date "2008-05-01" @default.
- W10383471 modified "2023-09-24" @default.
- W10383471 title "Synthesis, fluorine-18 labelling and radiopharmacological evaluation of F15599, a novel 5-HT1A receptor agonist" @default.
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