New fluoro-diphenylchalcogen derivatives to explore the serotonin transporter by PET

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4991-5. doi: 10.1016/j.bmcl.2007.02.082. Epub 2007 Mar 7.

Abstract

A series of fluorinated diphenylchalcogen derivatives, possessing a sulfur or an oxygen bridge, has been prepared with the aim to get a suitable radiotracer to image the SERT in vivo using positron emission tomography (PET). The compounds were synthesized and assayed toward the serotonin (SERT), dopamine (DAT), and norepinephrine (NET) transporters. Among the developed series, five compounds display a high SERT affinity (K(i): 0.27-2.91 nM range) and can be labeled either with carbon-11 or fluorine-18.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / drug effects
  • Chalcogens / chemical synthesis*
  • Chalcogens / chemistry
  • Chalcogens / pharmacology
  • Chemistry, Pharmaceutical / methods*
  • Dopamine / metabolism
  • Drug Design
  • Drug Evaluation, Preclinical
  • Humans
  • Hydrocarbons, Fluorinated / chemical synthesis*
  • Hydrocarbons, Fluorinated / chemistry
  • Hydrocarbons, Fluorinated / pharmacology
  • Models, Chemical
  • Norepinephrine / metabolism
  • Positron-Emission Tomography / methods*
  • Rats
  • Serotonin / metabolism
  • Serotonin Plasma Membrane Transport Proteins / chemistry*
  • Signal Transduction

Substances

  • Chalcogens
  • Hydrocarbons, Fluorinated
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin
  • Dopamine
  • Norepinephrine