[¹⁸F]FE@SNAP-A new PET tracer for the melanin concentrating hormone receptor 1 (MCHR1): microfluidic and vessel-based approaches

Bioorg Med Chem. 2012 Oct 1;20(19):5936-40. doi: 10.1016/j.bmc.2012.07.051. Epub 2012 Aug 7.

Abstract

Changes in the expression of the melanin concentrating hormone receptor 1 (MCHR1) are involved in a variety of pathologies, especially obesity and anxiety disorders. To monitor these pathologies in-vivo positron emission tomography (PET) is a suitable method. After the successful radiosynthesis of [(11)C]SNAP-7941-the first PET-Tracer for the MCHR1, we aimed to synthesize its [(18)F]fluoroethylated analogue: [(18)F]FE@SNAP. Therefore, microfluidic and vessel-based approaches were tested. [(18)F]fluoroethylation was conducted via various [(18)F]fluoroalkylated synthons and direct [(18)F]fluorination. Only the direct [(18)F]fluorination of a tosylated precursor using a flow-through microreactor was successful, affording [(18)F]FE@SNAP in 44.3 ± 2.6%.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Microfluidics* / methods
  • Piperidines / chemistry*
  • Positron-Emission Tomography* / methods
  • Pyrimidines / chemistry*
  • Receptors, Somatostatin / analysis*

Substances

  • Fluorine Radioisotopes
  • MCHR1 protein, human
  • Piperidines
  • Pyrimidines
  • Receptors, Somatostatin
  • SNAP7941