Mutagenic activity of a fluorinated analog of the beta-adrenoceptor ligand carazolol in the Ames test.
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.
Doze
P
P
PET Center, Groningen University Hospital, Groningen, The Netherlands. P.Doze@pet.azg.nl
Elsinga
P H
PH
de Vries
E F
EF
Van Waarde
A
A
Vaalburg
W
W
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis / Q000633:toxicity*; D000818:Animals; D005462:Fluorine Radioisotopes; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D009152:Mutagenicity Tests; D009153:Mutagens / Q000138:chemical synthesis / Q000633:toxicity*; D011412:Propanolamines / Q000633:toxicity*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000633:toxicity*; D051381:Rats; D017208:Rats, Wistar; D012486:Salmonella typhimurium / Q000187:drug effects / Q000235:genetics; D015430:Weight Gain / Q000187:drug effects
D000319:Adrenergic beta-Antagonists; D005462:Fluorine Radioisotopes; D008024:Ligands; D009153:Mutagens; D011412:Propanolamines; D019275:Radiopharmaceuticals; C014382:carazolol