Mutagenic activity of a fluorinated analog of the beta-adrenoceptor ligand carazolol in the Ames test

Nucl Med Biol. 2000 Apr;27(3):315-9. doi: 10.1016/s0969-8051(00)00087-1.

Abstract

S-1'[(18)F]-Fluorocarazolol (FCAR) is a fluorinated analog of the nonmutagenic beta-blocker carazolol (CAR). In former studies FCAR proved to be suitable for quantification of beta-adrenoceptors in vivo with positron emission tomography (PET). We report here that FCAR displays no acute toxicity in either rats or mice. However, FCAR induces a strong dose-related increase in the number of revertants in the Ames test. We conclude that FCAR yields mutagenic activity as measured by the Ames test.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis
  • Adrenergic beta-Antagonists / toxicity*
  • Animals
  • Fluorine Radioisotopes
  • In Vitro Techniques
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Mice
  • Mutagenicity Tests
  • Mutagens / chemical synthesis
  • Mutagens / toxicity*
  • Propanolamines / toxicity*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / toxicity*
  • Rats
  • Rats, Wistar
  • Salmonella typhimurium / drug effects
  • Salmonella typhimurium / genetics
  • Weight Gain / drug effects

Substances

  • Adrenergic beta-Antagonists
  • Fluorine Radioisotopes
  • Ligands
  • Mutagens
  • Propanolamines
  • Radiopharmaceuticals
  • carazolol