Synthesis and in silico evaluation of novel compounds for PET-based investigations of the norepinephrine transporter

Molecules. 2015 Jan 20;20(1):1712-30. doi: 10.3390/molecules20011712.

Abstract

Since the norepinephrine transporter (NET) is involved in a variety of diseases, the investigation of underlying dysregulation-mechanisms of the norepinephrine (NE) system is of major interest. Based on the previously described highly potent and selective NET ligand 1-(3-(methylamino)-1-phenylpropyl)-3-phenyl-1,3-dihydro-2H-benzimidaz- ol-2-one (Me@APPI), this paper aims at the development of several fluorinated methylamine-based analogs of this compound. The newly synthesized compounds were computationally evaluated for their interactions with the monoamine transporters and represent reference compounds for PET-based investigation of the NET.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Computer Simulation*
  • Humans
  • Ligands
  • Norepinephrine Plasma Membrane Transport Proteins / chemistry
  • Norepinephrine Plasma Membrane Transport Proteins / metabolism*
  • Positron-Emission Tomography*
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Reference Standards
  • Sequence Alignment

Substances

  • Ligands
  • Norepinephrine Plasma Membrane Transport Proteins
  • Radiopharmaceuticals