Rijks L J, Boer G J, Endert E, de Bruin K, Janssen A G, van Royen E A
Department of Nuclear Medicine, University of Amsterdam, The Netherlands.
Nucl Med Biol. 1997 Jan;24(1):65-75. doi: 10.1016/s0969-8051(96)00183-7.
The potential of both stereoisomers of 11 beta-methoxy-17 alpha-[123I] iodovinylestradiol (E- and Z-[123I]MIVE) as suitable radioligands for imaging of estrogen receptor (ER)-positive human breast tumours was studied. The 17 alpha-[123I]iodovinylestradiol derivatives were prepared stereospecifically by oxidative radioiododestannylation of the corresponding 17 alpha-tri-n-butylstannylvinylestradiol precursors. Both isomers of MIVE showed high in vitro affinity for dimethylbenzanthracene-induced rat and fresh human mammary tumour ER, that of Z-MIVE however being manyfold higher than that of E-MIVE. In vivo distribution studies with E- and Z-[123I]MIVE in normal and tumour-bearing female rats showed ER-mediated uptake and retention in uterus, ovaries, pituitary, hypothalamus and mammary tumours, again the highest for Z-[123I]MIVE. The uterus- and tumour-to-nontarget tissue (far, muscle) uptake ratios were also highest for Z-[123I]MIVE. Additionally, planar whole body imaging of two breast cancer patients 1-2 h after injection of Z-[123I]MIVE showed increased focal uptake at known tumour sites. Therefore, we conclude that Z-[123I]MIVE is a promising radioligand for the diagnostic imaging of ER in human breast cancer.
研究了11β-甲氧基-17α-[123I]碘乙烯雌二醇的两种立体异构体（E-和Z-[123I]MIVE）作为雌激素受体（ER）阳性人乳腺肿瘤成像合适放射性配体的潜力。通过相应的17α-三正丁基锡乙烯雌二醇前体的氧化放射性碘脱锡反应立体定向制备17α-[123I]碘乙烯雌二醇衍生物。MIVE的两种异构体对二甲基苯并蒽诱导的大鼠和新鲜人乳腺肿瘤ER均显示出高体外亲和力，然而Z-MIVE的亲和力比E-MIVE高许多倍。用E-和Z-[123I]MIVE在正常和荷瘤雌性大鼠中进行的体内分布研究表明，ER介导的摄取和保留存在于子宫、卵巢、垂体、下丘脑和乳腺肿瘤中，同样Z-[123I]MIVE的摄取和保留最高。Z-[123I]MIVE的子宫和肿瘤与非靶组织（脂肪、肌肉）摄取比也最高。此外，两名乳腺癌患者注射Z-[123I]MIVE后1-2小时的平面全身成像显示，已知肿瘤部位的局部摄取增加。因此，我们得出结论，Z-[123I]MIVE是用于人乳腺癌中ER诊断成像的一种有前景的放射性配体。
