16. cap alpha. -(/sup 77/Br)bromoestradiol-17. beta. : a high specific-activity, gamma-emitting tracer with uptake in rat uterus and induced mammary tumors

Journal Article · Wed Dec 31 23:00:00 EST 1980 · J. Nucl. Med.; (United States)

OSTI ID:6677486

Katzenellenbogen, J A ^[1]; Senderoff, S G; McElvany, K D; O'Brien, Jr, H A; Welch, M J

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1. Univ. of Illinois, Urbana

16..cap alpha..-(/sup 77/Br)bromoestradiol-17..beta.. (compound 1) has been synthesized by radiobromination of estrone enoldiacetate. Tissue uptake studies performed 1 hr after administration of compound 1 to immature or mature female rats showed uterus-to-blood ratios of 13, with nontarget tissue-to-blood ratios ranging from 0.6 to 2. Co-administration of unlabeled 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: 6677486
• 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

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
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551001 -- Physiological Systems-- Tracer Techniques
560172 -- Radiation Effects-- Nuclide Kinetics & Toxicology-- Animals-- (-1987)
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
AROMATICS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE 77
BROMINE ISOTOPES
CARCINOMAS
CHEMICAL PREPARATION
CHEMISTRY
CONDENSED AROMATICS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSIS
DIAGNOSTIC TECHNIQUES
DIAGNOSTIC USES
DIMETHYLBENZANTHRACENE
DISEASES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MAMMARY GLANDS
MATERIALS
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOACTIVE MATERIALS
RADIOCHEMISTRY
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
SCINTISCANNING
STEROID HORMONES
STEROIDS
SYNTHESIS
TISSUE DISTRIBUTION
USES
UTERUS
VERTEBRATES