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

J Med Chem. 2014 May 8;57(9):3884-90. doi: 10.1021/jm500372e. Epub 2014 Apr 29.

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, [(18)F]2FNQ1P, that possesses a high affinity and selectivity for 5-HT6. In vitro PET autoradiographies in rat brain sections with this radiotracer were in accordance with the 5-HT6 distribution pattern.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Cricetulus
  • Fluorine Radioisotopes / chemistry*
  • In Vitro Techniques
  • Positron-Emission Tomography*
  • Radioligand Assay
  • Receptors, Serotonin / chemistry
  • Receptors, Serotonin / metabolism*

Substances

  • Fluorine Radioisotopes
  • Receptors, Serotonin
  • serotonin 6 receptor