Estrogen receptor imaging with 17α-[123I]iodovinyl-11β-methoxyestradiol (MIVE2)—part I. Radiotracer preparation and characterization

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-04-01 DOI:10.1016/0883-2897(92)90108-B

C. Foulon , D. Guilloteau , J.L. Baulieu , M.J. Ribeiro-Barras , G. Desplanches , Y. Frangin , J.C. Besnard

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引用次数: 16

Abstract

It is important to know the estrogen receptor rate in breast carcinoma management. Thus, an in vivo and atraumatic method would be very useful. Different ligands have been proposed for this. We present here the specific synthesis of 20E- and 20Z-17α-iodovinyl-11β-methoxyestradiols and their biological characterization as estrogen receptor ligands. The two isomers were analysed by current chemical methods (NMR) and purified by HPLC. We carried out an in vivo study with 21-day-old Swiss mice to compare properties of the two ligands. The 20E-MIVE₂ showed the best affinity for estrogen receptors, the uterus-to-blood ratio was 15-fold higher for the trans derivative. We enhanced the in vivo and in vitro properties of the 20E-MIVE₂: the affinity constant was determined by Scatchard analysis, K_d = 16 × 10⁻¹⁰M, and biodistributions were performed with unlabelled estradiol pre-injection. We concluded that 20E-MIVE₂ can be used for a feasibility study in patients with breast carcinoma.

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雌激素受体的17α-[123I]碘乙烯基-11β-甲氧基雌二醇(MIVE2)成像-第一部分:放射性示踪剂的制备和表征

了解雌激素受体率对乳腺癌的治疗有重要意义。因此，一种体内无损伤的方法将是非常有用的。已经提出了不同的配体。本文报道了20E-和20z -17α-碘乙烯基-11β-甲氧基雌二醇的特异性合成及其作为雌激素受体配体的生物学特性。用现有的化学方法(核磁共振)对这两种异构体进行了分析，并用高效液相色谱对其进行了纯化。我们对21天大的瑞士小鼠进行了体内研究，以比较这两种配体的性质。20E-MIVE2对雌激素受体表现出最好的亲和力，其反式衍生物的子宫与血液比率高出15倍。我们增强了20E-MIVE2的体内和体外特性:通过Scatchard分析确定亲和力常数，Kd = 16 × 10−10M，并通过未标记雌二醇预注射进行生物分布。我们得出结论，20E-MIVE2可用于乳腺癌患者的可行性研究。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology

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