Simultaneous tritium labelling of two potent 5-HT4 ligands

Eur J Med Chem. 2010 Mar;45(3):1263-5. doi: 10.1016/j.ejmech.2009.12.012. Epub 2009 Dec 24.

Abstract

Two potent and selective 5-HT(4) ligands, [(3)H]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyridine (1a) and [(3)H]-1-methyl-5-[(N-propylpiperidin-4-yl)methoxy]pyrrolo[1,2-a]thieno[2,3-e]pyrazine (2a) were radiolabelled with tritium. Radioactive labelling was achieved by simultaneous tritium reduction of a mixture of both propargylic precursors (1c-2c). The two tritiated ligands thus obtained were radiochemically pure and possessed high radioactive specific activities. These tritiated 5-HT(4) ligands will allow for binding characterization as an essential tool for their further development.

MeSH terms

  • Ligands
  • Molecular Structure
  • Naphthyridines / chemistry*
  • Piperidines / chemistry*
  • Radiopharmaceuticals / chemistry*
  • Serotonin 5-HT1 Receptor Agonists*

Substances

  • ((3)H)-1-methyl-5-((N-propylpiperidin-4-yl)methoxy)pyrrolo(1,2-a)thieno(2,3-e)pyrazinenzo(h)(1,6)naphthyridine
  • ((3)H)-5-((N-propylpiperidin-4-yl)methoxy)-1,2,3,4-tetrahydrobenzo(h)(1,6) naphthyridine
  • Ligands
  • Naphthyridines
  • Piperidines
  • Radiopharmaceuticals
  • Serotonin 5-HT1 Receptor Agonists