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

被引:14
作者
Doze, P [1 ]
Elsinga, PH [1 ]
de Vries, EFJ [1 ]
Van Waarde, A [1 ]
Vaalburg, W [1 ]
机构
[1] Univ Groningen Hosp, PET Ctr, NL-9700 RB Groningen, Netherlands
关键词
PET; mutagenicity; beta-adrenoceptors; fluorine introduction;
D O I
10.1016/S0969-8051(00)00087-1
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
S-1'[F-18]-Fluorocarazolol (FCAR) is a fluorinated analog of the nonmutagenic beta-blocker carazolol (CAR). Tn 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. NUCL MED BIOL 27;3:315-319, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:315 / 319
页数:5
相关论文
共 24 条
[1]   METHODS FOR DETECTING CARCINOGENS AND MUTAGENS WITH SALMONELLA-MAMMALIAN-MICROSOME MUTAGENICITY TEST [J].
AMES, BN ;
MCCANN, J ;
YAMASAKI, E .
MUTATION RESEARCH, 1975, 31 (06) :347-363
[2]   GENETIC TOXICOLOGY - CAN WE DESIGN PREDICTIVE INVIVO ASSAYS [J].
CLIVE, D .
MUTATION RESEARCH, 1988, 205 (1-4) :313-330
[3]   (S,S)- and (S,R)-1'-[F-18]fluorocarazolol, ligands for the visualization of pulmonary beta-adrenergic receptors with PET [J].
Elsinga, PH ;
Vos, MG ;
vanWaarde, A ;
Braker, AH ;
deGroot, TJ ;
Anthonio, RL ;
Weemaes, AMA ;
Brodde, OE ;
Visser, GM ;
Vaalburg, W .
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (02) :159-167
[4]   Toxicity, mutagenicity, and behavioral effects of β-CIT, a ligand for dopamine transporter exploration by SPECT [J].
Emond, P ;
Farde, L ;
Chalon, S ;
Belzung, C ;
Mauclaire, V ;
Chiron, JP ;
Halldin, C ;
Besnard, JC ;
Guilloteau, D .
NUCLEAR MEDICINE AND BIOLOGY, 1998, 25 (04) :405-409
[5]  
*EUR COMM, 1997, IP97636 EUR COMM, P1
[6]  
GREGORY NG, 1982, VET RES COMMUN, V5, P277
[7]   CARCINOGENICITY OF ALDERLIN (PRONETHALOL) IN MICE [J].
HOWE, R .
NATURE, 1965, 207 (4997) :594-&
[8]   MUTAGENICITY OF ENANTIOMERS OF PENBUTOLOL [J].
HUSSAIN, SS ;
ABOULENEIN, HY ;
ALDAKAN, A ;
HANNAN, MA .
DRUG AND CHEMICAL TOXICOLOGY, 1989, 12 (01) :77-83
[9]   DNA STRAND BREAKS AND MUTATIONS CAUSED BY PENBUTOLOL, A BETA-BLOCKER [J].
HUSSAIN, SS ;
ALDAKAN, AA ;
ABOULENEIN, HY ;
HANNAN, MA .
MUTATION RESEARCH, 1988, 204 (04) :675-682
[10]   A TOXICOLOGICAL REVIEW OF BETA-ADRENERGIC BLOCKERS [J].
JACKSON, CD ;
FISHBEIN, L .
FUNDAMENTAL AND APPLIED TOXICOLOGY, 1986, 6 (03) :395-422