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

P Doze; P H Elsinga; E F de Vries; A Van Waarde; W Vaalburg

doi:10.1016/s0969-8051(00)00087-1

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.

Authors

P Doze¹, P H Elsinga, E F de Vries, A Van Waarde, W Vaalburg

Affiliation

¹ PET Center, Groningen University Hospital, Groningen, The Netherlands. [email protected]

PMID: 10832089
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