Delpassand E S, Yang D J, Wallace S, Cherif A, Quadri S M, Price J, Joubert A, Inoue T, Podoloff D A
Division of Diagnostic Imaging, University of Texas M. D. Anderson Cancer Center, Houston 77030, USA.
J Pharm Sci. 1996 Jun;85(6):553-9. doi: 10.1021/js960049w.
This study was aimed at developing a hydrophilic diethylenetriaminepentaacetic acid-tamoxifen (DTPA-Tam) analogue for use in imaging estrogen receptor positive (ER+) lesions. In rat uterine cytosol, the IC50 of DTPA-Tam conjugate was 1 microM and of tamoxifen, 2 microM. Biodistribution, autoradiography, and radionuclide imaging of 111In-DTPA-Tam in breast-tumor-bearing rats showed that tumor-to-tissue ratios increased steadily between 30 min and 48 h. The in vivo response of MCF-7 breast cancer xenografts to tamoxifen and DTPA-Tam in nude mice demonstrated that DTPA-Tam could reduce tumor growth rate. These results indicate that DTPA-Tam, a new hydrophilic ER+ ligand, might be useful in diagnosing ER+ lesions.
本研究旨在开发一种亲水性二乙烯三胺五乙酸-他莫昔芬（DTPA-Tam）类似物，用于对雌激素受体阳性（ER+）病变进行成像。在大鼠子宫胞质溶胶中，DTPA-Tam偶联物的IC50为1微摩尔/升，他莫昔芬的IC50为2微摩尔/升。对荷乳腺肿瘤大鼠体内111In-DTPA-Tam的生物分布、放射自显影和放射性核素成像显示，肿瘤与组织的比率在30分钟至48小时之间稳步增加。MCF-7乳腺癌异种移植瘤在裸鼠体内对他莫昔芬和DTPA-Tam的反应表明，DTPA-Tam可降低肿瘤生长速率。这些结果表明，新型亲水性ER+配体DTPA-Tam可能有助于诊断ER+病变。
