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16 alpha-(/sup 77/Br)bromo-11 beta-methoxyestradiol-17 beta: a gamma-emitting estrogen imaging agent with high uptake and retention by target organs

Journal Article · · J. Nucl. Med.; (United States)
OSTI ID:6816773
; ; ; ; ;

16 alpha(/sup 77/Br)Bromo-11 beta-methoxyestradiol-17 beta (MBE(/sup 77/Br)), a compound with high affinity for the estrogen receptor and with low nonspecific binding, has been prepared with an effective specific activity of 770--1450 Ci per mmole at the time of synthesis. In immature female rats, this compound is taken up selectively by the uterus and is retained for prolonged periods. This is presumably due to the binding of this compound to the estrogen receptor, as uterine uptake is blocked selectively by coadministration of an excess of unlabeled estradiol, and administration of a chase dose of unlabeled estradiol results in a rapid decrease in activity in the uterus. In double-label experiments with 16 alpha(/sup 125/I)estradiol and MBE(/sup 77/Br), the two compounds showed equally selective uterine uptake at 1 hr, but the bromine-labeled compound became increasingly more selective at 3 and 6 hr. MBE(/sup 77/Br) may prove to be a more favorable agent for imaging human breast tumors than our previously described compound, 16 alpha-(/sup 77/Br)bromoestradiol-17 beta.

Research Organization:
University of Illinois, Urbana
OSTI ID:
6816773
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 23:5; ISSN JNMEA
Country of Publication:
United States
Language:
English

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In vivo comparison of 16. cap alpha. -(/sup 77/Br)bromoestradiol-17. beta. and 16. cap alpha. -(/sup 125/I)Iodoestradiol-17. beta
Journal Article · Sat May 01 00:00:00 EDT 1982 · J. Nucl. Med.; (United States) · OSTI ID:7007018
In vivo comparison of 16 alpha(/sup 77/Br)bromoestradiol-17 beta and 16 alpha-(/sup 125/I)iodoestradiol-17 beta
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Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BROMINE 77
BROMINE ISOTOPES
CARCINOMAS
COMPARATIVE EVALUATIONS
DAYS LIVING RADIOISOTOPES
DIAGNOSIS
DIAGNOSTIC USES
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MAMMARY GLANDS
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PATIENTS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
UPTAKE
USES
UTERUS
VERTEBRATES