A correlative study between 99mTc-ESTCPTA and 99mTc-MIBI in rats

Tissue distribution of the 99mTc labeled derivative of the estrogen compound 3,17-alpha-estradiolyl propyl 1,4,8,11-tetraazacyclotetradecanyl-l-(4-methylbenzoic acid) ester (ESTCPTA), which has an 3,17-alpha-estradiolyl propinol coupled to l-(4-methylbenzoic acid)1,4,8,11-tetraazacyclotetradecane (CPTA), was compared to 99mTc-MIBI (methoxyisobutyl isonitrile) in female Albino Wistar rats. Tissues of interest included lung, liver, heart, kidneys, spleen, stomach, intestines, pancreas, muscle, blood, breast, ovary, fat, and uterus. 99mTc-ESTCPTA uptake by the uterus and ovary, as ER-rich tissues, was highly selective. Maximum uptakes for 99mTc-MIBI and 99mTc-ESTCPTA are 90 min in breast, ovary and uterus. The pancreas also showed significant receptor saturated and unsaturated ratios for 99mTc-ESTCPTA. Results are sufficiently encouraging to generate further evaluation of these and related compounds as possible estrogen receptor based tumor imaging and therapeutic agents in estrogen-rich tissues.