Receptor-binding radiopharmaceuticals for imaging breast tumors: estrogen-receptor interactions and selectivity of tissue uptake of halogenated estrogen analogs

Conference · Sun Jun 01 00:00:00 EDT 1980 · J. Nucl. Med.; (United States)

OSTI ID:5298972

Katzenellenbogen, J A; Carlson, K E; Heiman, D F; Goswami, R

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), Journal Name: J. Nucl. Med.; (United States) Vol. 21:6; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702 -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
560172* -- Radiation Effects-- Nuclide Kinetics & Toxicology-- Animals-- (-1987)
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL LOCALIZATION
BODY
CHEMICAL BONDS
CHEMICAL PREPARATION
CHEMISTRY
DATA
DATA FORMS
DISEASES
DRUGS
ESTRADIOL
ESTRANES
ESTROGENS
EXPERIMENTAL DATA
FEMALE GENITALS
GLANDS
GRAPHS
HORMONES
HYDROGEN ISOTOPES
HYDROXY COMPOUNDS
IMAGES
INFORMATION
ISOTOPES
LABELLED COMPOUNDS
LABELLING
LIGHT NUCLEI
MAMMALS
MAMMARY GLANDS
NEOPLASMS
NUCLEI
NUMERICAL DATA
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANS
RADIOACTIVE MATERIALS
RADIOCHEMISTRY
RADIOISOTOPES
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
SYNTHESIS
TABLES
TRITIUM
TRITIUM COMPOUNDS
UPTAKE
UTERUS
VERTEBRATES
YEARS LIVING RADIOISOTOPES