Radiopharmaceuticals comprising molecules that target to N-formyl-methionyl-leucyl-phenylalanine (fMLF) receptor on leukocytes in order to target sites of inflammation for diagnostic imaging are described. The targeting molecules are attached to capping groups that make the entire molecule either antagonists or weak agonists of fMLF receptor and therefore do not elicit a chemotactic response resulting in neutropenia. The preferred targeting molecule is ReO-Gly-lys(Dimethylgly-t-Butylgly-cys-gly)-glu-trp-phe-leu-nle-NHCOcyclopropyl. The invention also relates to the use of combinatorial chemistry to obtain preferred molecules that target sites of inflammation for diagnostic imaging.
本研究描述了由靶向白细胞上的 N-甲酰基-蛋
氨酰-
亮氨酰-苯丙氨酸(fMLF)受体的分子组成的放射性药物,以便针对炎症部位进行诊断成像。靶向分子附有封端基团,使整个分子成为 fMLF 受体的拮抗剂或弱激动剂,因此不会引起导致中性粒细胞减少的趋化反应。优选的靶向分子是 ReO-Gly-lys(Dimethylgly-t-Butylgly-cys-gly)-glu-trp-phe-leu-nle-NHCOcyclopropyl。本发明还涉及使用组合
化学方法获得优选的靶向炎症部位的分子,用于诊断成像。