Receptor-binding radiopharmaceuticals for imaging breast tumors: estrogen-receptor interactions and selectivity of tissue uptake of halogenated estrogen analogs
Four halogenated estrogen analogs - o-fluorohexestrol, and 1-fluoro-, 1-bromo-, and 1-iodohexestrol - have been prepared and tritium-labeled in high specific activity, to investigate their potential as estrogen-receptor-based agents for imaging breast tumors. These compounds bind with high affinity in vitro to the cytoplasmic uterine estrogen receptor from rat and lamb and sediment as 8S receptor complexes on sucrose gradients. After 1 hr in immature rats, these compounds show high uptake into the uterus, but low uptakes (10 to 25% of the uterine levels) into most nontarget tissues. The uterine uptake is estrogen specific since it is depressed by excess nonradioactive estradiol. Uptake selectivity is greatest for the fluorohexestrols and decreases for the bromo and iodo compounds. In mature rats bearing DMBA-induced mammary tumors, selective uptake by the uterus and tumors is seen with 1-fluoro(/sup 3/H/sub 4/)hexestrol and o-fluoro(/sup 3/H/sub 3/)hexestrol. The studies indicate that these four halogenated hexestrols are promising candidates as estrogen-receptor-based agents for the imaging of human breast tumors.
- Research Organization:
- Univ. of Illinois, Urbana
- OSTI ID:
- 5298972
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 21:6; Conference: 27. annual meeting of the Society of Nuclear Medicine, Detroit, MI, USA, 24 Jun 1980
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
ESTRADIOL
LABELLING
ESTROGENS
RECEPTORS
MAMMARY GLANDS
RADIONUCLIDE KINETICS
NEOPLASMS
ORGANIC HALOGEN COMPOUNDS
CHEMICAL BONDS
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
TRITIUM COMPOUNDS
BIOLOGICAL LOCALIZATION
RADIOCHEMISTRY
UPTAKE
UTERUS
EXPERIMENTAL DATA
GRAPHS
IMAGES
RATS
TABLES
TRITIUM
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CHEMISTRY
DATA
DATA FORMS
DISEASES
DRUGS
ESTRANES
FEMALE GENITALS
GLANDS
HORMONES
HYDROGEN ISOTOPES
HYDROXY COMPOUNDS
INFORMATION
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MAMMALS
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOACTIVE MATERIALS
RADIOISOTOPES
RODENTS
STEROID HORMONES
STEROIDS
SYNTHESIS
VERTEBRATES
YEARS LIVING RADIOISOTOPES
560172* - Radiation Effects- Nuclide Kinetics & Toxicology- Animals- (-1987)
550601 - Medicine- Unsealed Radionuclides in Diagnostics
400702 - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials