新型肾上腺显影剂——6-(^(82)Br)溴甲基胆固醇的合成及其在动物组织内的分布

NEW CHOLESTEROL ANALOGUE AS ADRENAL IMAGING AGENT——SYNTHESIS AND TISSUE DISTRIBUTION OF BROMINE-82 LABELED 6-BROMOMETHYL CHOLESTEROL

自从1968年Nagai等首次将^(131)I标记胆固醇作为肾上腺示踪剂以来,1970年Counsell等报道了19-(^(131)I)碘胆固醇的合成和在动物肾上腺中有明显的浓集。1975年Kojima等制备了6-(^(131)I)碘甲基去甲胆固醇,动物实验表明它具有更高的亲肾上腺组织特性。其后,王世真、刘伯里等研制了6-(^(131)I)碘胆固醇,显示有较好的亲肾上腺功能和更为优良的热稳定性和辐射稳定性。为了寻找更佳的肾上腺显影剂。

6-Bromomethyl cholesterol (CL-6-MeBr) is synthesized from cholesterol by six step reactions. Bromine-82 labeled 6-bromomethyl cholesterol (CL-6-MeBr-82) is prepared by means of hydrothermal melting method. Tissue distribution of CL-6-MeBr-82 in mice is determined. The adrenal uptake of CL-6-MeBr-82 reaches a maximum of 92.08% dose/g at the 5th day after injection, and the adrenal to liver ratio increases from 4.2 at 1 day to 48.72 at five days.CL-6-MeBr-82 shows less affinity for the adrenal gland than CL-6-Br-82.