Syntheses, Radiolabelings, and in Vitro Evaluations of Fluorinated PET Radioligands of 5?HT_6 Serotoninergic Receptors

摘要

The 5-HT_6 receptors are potent therapeutic targets for psychiatric and neurological diseases (schizophrenia, Alzheimer’s disease, etc.). However, with lack of specific radiopharmaceuticals, their pharmacology is still incomplete and their exploration is limited to animal models. In this context, we have designed a fluorinated PET radiotracer, [~(18)F]2FNQ1P, that possesses a high affinity and selectivity for 5-HT_6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT_6 distribution pattern.