131I labeling of tamoxifen and biodistribution studies in rats.
Tamoxifen [TAM ([Z]-2-[4-(1,2-diphenyl-1-di-butenyl)-phenoxy]-N,N-dimethylethanamine)] has been used as an antiestrogen drug for treatment and prevention of human breast cancer. Tamoxifen was labeled with 131I using iodogen as an oxidizing agent. Mass spectroscopy of the cold standard showed that the labeling occurs in ortho position to the phenyl ether position of TAM as expected. Quality control, radiochemical yield and stability were established using the radioelectrophoresis method. The radiolabeled compound maintained its stability throughout working period of 24 h. Scintigraphic imaging was performed and tissue distribution was determined in Albino Wistar rats. According to biodistribution and imaging experiments the radiolabeled compound presented estrogen receptor (ER) specificity and it was uptaken by endometrium as well as breast tissue.
Muftuler
F Z Biber
FZ
Department of Nuclear Applications, Institute of Nuclear Sciences, Ege University, Bornova-Izmir, Turkey. fazilet.zumrut.biber@ege.edu.tr
Unak
P
P
Teksoz
S
S
Acar
C
C
Yolcular
S
S
Yürekli
Y
Y
D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes / Q000097:blood / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D020845:Selective Estrogen Receptor Modulators / Q000097:blood / Q000493:pharmacokinetics; D013629:Tamoxifen / Q000097:blood / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D020845:Selective Estrogen Receptor Modulators; D013629:Tamoxifen