Syntheses, radiolabelings, and in vitro evaluations of fluorinated PET radioligands of 5-HT6 serotoninergic receptors

J Colomb, G Becker, S Fieux, L Zimmer…

Index: Colomb, Julie; Becker, Guillaume; Fieux, Sylvain; Zimmer, Luc; Billard, Thierry Journal of Medicinal Chemistry, 2014 , vol. 57, # 9 p. 3884 - 3890

Full Text: HTML

Citation Number: 13

Abstract

The 5-HT6 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,[18F] 2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET ...