18F-labeled sufentanil for PET-imaging of mu-opioid receptors

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1773-7. doi: 10.1016/j.bmcl.2005.02.049.

Abstract

The synthesis of an (18)F-labeled sufentanil analogue with apparent high mu-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenyl-2-(+/-)-[(18)F]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the mu-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in mu-opioid receptor mapping and quantitation with positron emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism
  • Fluorine Radioisotopes*
  • Mice
  • Positron-Emission Tomography / methods
  • Radiopharmaceuticals / metabolism*
  • Receptors, Opioid, mu / metabolism*
  • Sufentanil / analogs & derivatives
  • Sufentanil / metabolism*

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Opioid, mu
  • Sufentanil