Metabolism of alpha-methylfluorene-2-acetic acid (cicloprofen): isolation and identification of metabolites from rat urine

Xenobiotica. 1978 Feb;8(2):121-31. doi: 10.3109/00498257809060391.

Abstract

1. Four metabolites of alpha-methylfluorene-2-acetic acid (cicloprofen) have been isolated from rat urine and identified as the 7-hydroxy, 9-hydroxy, 7,9-dihydroxy and 9-hydroxy-9-methoxy derivatives of cicloprofen. 2. 7-Hydroxy cicloprofen was the major metabolite, contributing 47% of the total radioactivity excreted in rat urine. The other three metabolites each contributed approx. 10% of the radioactivity in urine. There was little unchanged drug excreted in urine (2-6%); at least three other minor metabolites have not been identified. 3. A metabolic pathway for the formation of the 9-hydroxy-9-methoxy metabolite of cicloprofen is proposed.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / urine*
  • Chromatography, Thin Layer
  • Fluorenes / isolation & purification
  • Fluorenes / urine
  • Hydroxylation
  • Magnetic Resonance Spectroscopy
  • Male
  • Mass Spectrometry
  • Propionates / isolation & purification
  • Propionates / urine*
  • Rats

Substances

  • Anti-Inflammatory Agents
  • Fluorenes
  • Propionates