16 alpha-(/sup 77/Br)bromoestradiol-17 beta: a high specific-activity, gamma-emitting tracer with uptake in rat uterus and uterus and induced mammary tumors
16 alpha-(77Br)bromoestradiol-17 beta (Compound 1) has been synthesized by radiobromination of estrone enoldiacetate. Tissue uptake studies performed 1 h after administration of Compound 1 to immature or mature female rats showed uterus-to-blood ratios of 13, with nontarget issue-to-blood ratios ranging from 0.6 to 2. Co-administration of unlabelled estradiol caused a selective depression in the uterine uptake with no effect on nontarget tissue uptake. In adult animals bearing adenocarcinomas induced by DMBA (7,12-dimethylbenz(a)anthracene), tumor-to-blood ratios of 6.3 were obtained, this uptake also being depressed in animals treated with unlabeled estradiol. The studies demonstrate that Compound 1 has suitable binding properties and sufficiently high specific activity so that its uptake in estrogen target tissues in vivo is mediated primarily by the estrogen receptor. Furthermore, they suggest that this compound may be suitable for imaging human breast tumors that contain estrogen receptors.
- OSTI ID:
- 6113490
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 22:1
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
BROMINE 77
UPTAKE
ESTRADIOL
MAMMARY GLANDS
RADIONUCLIDE KINETICS
NEOPLASMS
UTERUS
ADENOMAS
BROMINATION
DIMETHYLBENZANTHRACENE
LABELLED COMPOUNDS
RATS
TRACER TECHNIQUES
ANIMALS
AROMATICS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE ISOTOPES
CHEMICAL REACTIONS
CONDENSED AROMATICS
DAYS LIVING RADIOISOTOPES
DISEASES
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HALOGENATION
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
MINUTES LIVING RADIOISOTOPES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RODENTS
STEROID HORMONES
STEROIDS
VERTEBRATES
560172* - Radiation Effects- Nuclide Kinetics & Toxicology- Animals- (-1987)