Biodistribution of 123I-labeled 4-hydroxytamoxifen derivatives in rats with dimethylbenzanthracene-induced mammary carcinomas

Nuclear Medicine and Biology

Volumn 24, Issue 8, 1997, Pages 719-722

  Kruijer, Perry S ^a   Klok, Rob P ^a   Van Den Koedijk, Christa D M A ^b   Blankenstein, Marinus A ^b   Voskuil, Jan Henk ^c   Verzeijlbergen, J Fred ^c   Ensing, Geert J ^d   Herscheid, Jacobus D M ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

^b UNIVERSITY MEDICAL CENTER UTRECHT   (Netherlands)

^c ST ANTONIUS HOSPITAL   (Netherlands)

^d Mallinckrodt Medical BV   (Netherlands)

Author keywords

123I labeling; AEBS; Tamoxifen

Indexed keywords

4 HYDROXYTAMOXIFEN; 4 HYDROXYTAMOXIFEN I 123; ESTROGEN; ESTROGEN RECEPTOR; IODINE 123; UNCLASSIFIED DRUG; 4-HYDROXYTAMOXIFEN; 7,12 DIMETHYLBENZ[A]ANTHRACENE; ANTIESTROGEN; CARCINOGEN; DIAGNOSTIC AGENT; DRUG DERIVATIVE; RADIOACTIVE IODINE; RADIOPHARMACEUTICAL AGENT; TAMOXIFEN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING SITE; BREAST CARCINOMA; DRUG DISTRIBUTION; FEMALE; ISOTOPE LABELING; NONHUMAN; RAT; ANIMAL; CHEMICALLY INDUCED DISORDER; CHEMISTRY; EXPERIMENTAL NEOPLASM; METABOLISM; SYNTHESIS; TISSUE DISTRIBUTION; WISTAR RAT;

9,10-DIMETHYL-1,2-BENZANTHRACENE; ANIMALS; BINDING SITES; CARCINOGENS; ESTROGEN ANTAGONISTS; FEMALE; IODINE RADIOISOTOPES; MAMMARY NEOPLASMS, EXPERIMENTAL; RADIOPHARMACEUTICALS; RATS; RATS, WISTAR; TAMOXIFEN; TISSUE DISTRIBUTION;

EID: 0030608675     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(97)00111-X     Document Type: Article

References (15)

1. Blankenstein M. A., Peters-Mechielsen M. J., Mulder E. and Van der Molen H. J. (1980) Estimation of total oestrogen receptors in DMBA-induced rat mammary tumours by exchange of nuclear bound ligand at low temperature: A comparison with rat uterus. J. Steroid Biochem. 13, 557-564.
2. Blankenstein M. A., Van Woudenberg A. and Thijssen J. H. H. (1986) Occurrence and ligand specificity of anti-oestrogen binding sites (AEBS) in human breast tumor and uterine tissue. In: Endocrinology and Malignancy: Basic and Clinical Issues: Proceedings of the First International Congress on Cancer and Hormones, Rome, Italy, 1986 (Edited by Baulieu E. E., Iacobelli S. and McGuire W. L), pp. 387-394. The Parthenon Publishing Group, Carnforth, UK.
3. Coenen H. H., Moerlein S. M. and Stöcklin G. (1983) No-carrier added radiohalogenation methods with heavy halogens. Radiochim. Acta 34, 47-68.
4. Katzenellenbogen J. A., Heiman D. F., Carlson K. E. and Lloyd J. E. (1982) In vivo and in vitro steroid receptor assays in the design of estrogen radiopharmaceuticals. In: Receptor Binding Radiotracers, Vol. 1 (Edited by Eckelman W. C.), pp. 93-126. CRC Press, Boca Raton. FL.
5. McCague R. (1989) Iodotamoxifen derivatives and use for estrogen receptor-positive breast cancer detection and therapy. U. S. Patent 4 839, 155.
6. McCague R. and Potter G. A. (1994) Synthesis of 4-stannylated tamoxifen analogues: Useful precursors to radiolabelled iodoxifen and aziridinyl 4-iodotamoxifen. J. Label. Cmpd. Radiopharm. 34, 297-302.
7. 123I radioiodination of 15(p-I-phenyl)-9-methyl pentadecanoic acid, a potential myocardial tracer. Eur. J. Nucl. Med. 13, 159-160.
8. Moerlein S. M., Beyer W. and Stöcklin G. (1988) No-carrier-added radiobromination and radioiodination of aromatic rings with in situ generated peracetic acid. J. Chem. Soc. Perkins Trans. 1, 779-786.
9. Robertson D. W., Katzenellenbogen J. A., Long D. J., Rorke E. A. and Katzenellenbogen B. S. (1982) Tamoxifen antiestrogens: A comparison of the activity, pharmacokinetics and metabolic activation of the cis and trans isomers of tamoxifen. J. Steroid Biochem. 16, 1-13.
10. Simpson D. M., Elliston J. F. and Katzenellenbogen J. A. (1987) Desmethylnafoxidine aziridine: An electrophilic affinity label for the estrogen receptor with high efficiency and selectivity. J. Steroid Biochem. 28, 233-245.
11. Sutherland R. L., Murphy L. C., Foo M. S., Green M. D. and Whybourne A. M. (1980) High affinity anti-oestrogen binding site distinct from oestrogen receptor. Nature 288, 273-275.
12. Trivedi M., Potter G., Hammersley P., Carnochan P., Young H., Jarman M. and Ott R. (1995) NCA radioiodination of iodoxifen. J. Label. Cmpd. Radiopharm. 36, 921-926.
13. Van den Koedijk C. D. M. A., Kruijer P. S., Blankenstein M. A., Moret E. E., Van der Draai I., Voskuil J.-H., Ensing G. J. and Herscheid J. D. M. (1994) Synthesis of brominated 4-hydroxytamoxifen derivatives and QSAR of triphenylethylene compounds for the rat liver antioestrogen binding site and for the human myometrium oestrogen receptor. In: Antioestrogen Binding Sites (Edited by van den Koedijk C. D. M. A.), pp. 41-68. Utrecht University, Utrecht.
14. 125I-labeled cholinergic nerve marker (-)-5-iodobenzovesamicol. Nucl. Med. Biol. 20, 927-937.
15. Young H., Carnocan P., Trivedi M., Potter G. A., Eccles S. A., Haynes B. P., Jarman M. and Ott R. J. (1995) Pharmacckinetics and biodistribution of radiolabelled iodoxifen: Prospects for the use of PET in the evaluation of a novel antioestrogen for cancer therapy. Nucl. Med. Biol. 22, 405-411.