ESTROGEN RECEPTOR-BASED AGENTS FOR IMAGING BREAST TUMORS: BINDING SELECTIVITY AS A BASIS FOR DESIGN AND OPTIMIZATION

摘要: Abstract The presence of estrogen receptors in the majority human breast tumors provides an opportunity for selective localization γ-emitting estrogens. It is necessary that radiopharmaceuticals be prepared with high specific activity (1000 Ci/mmole), and they have both affinity receptor as well low non-receptor proteins. binding selectivity index (BSI) radiopharmaceutical defined ratio its to BSI any new compound can evaluated by a combination vitro measurements calculations based on octanol-water partition coefficients. We several steroidal non-steroidal analogues, bearing halogen substituents non-radiolabeled form, we radiolabeled form those whose was high. agents show highly uptakes uterus DMBA-induced mammary rats. target tissue uptake (determined vivo ) parallels closely measured vitro. Receptor alone, however, poor predictor selectivity. Images rats were observed 16- 77 Br-bromoestradiol.