Quantification of the radio-metabolites of the serotonin-1A receptor radioligand [carbonyl-11C]WAY-100635 in human plasma: an HPLC-assay which enables measurement of two patients in parallel

Appl Radiat Isot. 2012 Dec;70(12):2730-6. doi: 10.1016/j.apradiso.2012.08.016. Epub 2012 Sep 13.

Abstract

[Carbonyl-(11)C]WAY-100635 is a potent and effective antagonist for the 5-HT(1A) receptor subtype. We aimed to assess the status of [carbonyl-(11)C]WAY-100635 and its main radio-metabolites, [carbonyl-(11)C]desmethyl-WAY-100635 and [carbonyl-(11)C]cyclohexanecarboxylic acid, on the basis of an improved radio-HPLC method. Common methods were characterized by preparative HPLC columns with long runtimes and/or high flow rates. Considering the short half-life of C-11, we developed a more rapid and solvent saving HPLC assay, allowing a fast, efficient and reliable quantification of these major metabolites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chromatography, High Pressure Liquid / methods
  • Humans
  • Piperazines / blood
  • Piperazines / isolation & purification
  • Piperazines / metabolism*
  • Pyridines / blood
  • Pyridines / isolation & purification
  • Pyridines / metabolism*
  • Receptor, Serotonin, 5-HT1A / metabolism*
  • Serotonin 5-HT1 Receptor Antagonists / metabolism

Substances

  • Piperazines
  • Pyridines
  • Serotonin 5-HT1 Receptor Antagonists
  • desmethyl-WAY 100635
  • Receptor, Serotonin, 5-HT1A
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide