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

Journal Article · Thu Jan 01 04:00:00 EST 1981 · J. Nucl. Med.; (United States)

OSTI ID:6113490

Katzenellenbogen, J A; Senderoff, S G; McElvany, K D; O'Brien, Jr, H A; Welch, M J

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), Journal Name: J. Nucl. Med.; (United States) Vol. 22:1; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

560172* -- Radiation Effects-- Nuclide Kinetics & Toxicology-- Animals-- (-1987)
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ADENOMAS
ANIMALS
AROMATICS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINATION
BROMINE 77
BROMINE ISOTOPES
CHEMICAL REACTIONS
CONDENSED AROMATICS
DAYS LIVING RADIOISOTOPES
DIMETHYLBENZANTHRACENE
DISEASES
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HALOGENATION
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MAMMARY GLANDS
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RADIONUCLIDE KINETICS
RATS
RODENTS
STEROID HORMONES
STEROIDS
TRACER TECHNIQUES
UPTAKE
UTERUS
VERTEBRATES