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测定乳腺癌雌激素受体含量的诊断剂不仅能指明合适的治疗方法,还能识别各病程阶段。为此目的发展的放射性示踪剂应具有对雌激素受体的高度亲和性和高度体内稳定性。根据报道过的在体内代谢最小和非受体结合最少的化合物——甲氧基乙炔雌醇,合成了其衍生物17α-(E)-2-[~(135)Ⅰ]碘代乙烯基雌-1,3,5(10)-三烯-3,17β-二醇(~(125)Ⅰ-MIVE_2),其中放射性碘结合在21位碳上,作为稳定的碘代乙烯基衍生物,并测定了它的体内外特性。K_A和比活性:用从未成年大鼠子宫得到的雌激素受体测定。制备物的比放射性为1890 Ci/mmol,K_A值为6.8×10~9M-1,非受体结合不超过总量的5%。
Diagnostic agents that measure estrogen receptor levels in breast cancer not only identify the appropriate treatment but also identify stages of disease. Radiotracers developed for this purpose should have a high affinity for the estrogen receptor and a high degree of in vivo stability. Derivatives of 17α- (E) -2- [~ (135) I] iodo-vinylnaphthalene were synthesized according to the reported compound, methoxyethynyl estradiol, which has the lowest metabolism in the body and non-receptor binding -1,3,5 (10) -triene-3,17β-diol (~ (125) I-MIVE_2), in which radioactive iodine binds to carbon 21 as a stable iodovinyl derivative and Its in vitro and in vivo properties were determined. K_A and specific activity: The estrogen receptor assay obtained from the uterus of a juvenile rat. The specific activity of the preparation was 1890 Ci / mmol, the K_A value was 6.8 × 10 -9 M -1, and the non-receptor binding did not exceed 5% of the total amount.