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Estrogen receptor binding radiopharmaceuticals: II. Tissue distribution of 17. cap alpha. -methylestradiol in normal and tumor-bearing rats

Journal Article · · J. Nucl. Med.; (United States)
OSTI ID:5692616
; ; ; ; ; ; ;
Tritiated 17..cap alpha..-methylestradiol was synthesized to investigate the potential of the carbon-11-labeled analog as an estrogen-receptor-binding radiopharmaceutical. In vitro, 17..cap alpha..-methylestradiol is bound with high affinity to the cytoplasmic estrogen receptor from rabbit uterus (K/sub d/ = 1.96 x 10/sup -10/M), and it sediments as an 8S hormone-receptor complex in sucrose gradients. The compound shows specific uptake in the uterus of the adult rat, within 1 h after injection. In female rats bearing DMBA-induced tumors, specific uterine and tumor uptakes were observed, although at 30 min the tumor uptake was only 23 to 30% of the uptake in the uterus. Tritiated 17..cap alpha..-methylestradiol with a specific activity of 6 Ci/mmole showed a similar tissue distribution. Our results indicate that a 17 ..cap alpha..-methylestradiol is promising as an estrogen-receptor-binding radiopharmaceutical.
Research Organization:
Univ. Hospital, Groningen, Netherlands
OSTI ID:
5692616
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 24:6; ISSN JNMEA
Country of Publication:
United States
Language:
English

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Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702* -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BODY
CHEMICAL PROPERTIES
DATA
DISEASES
DISTRIBUTION
DRUGS
ESTROGENS
EXPERIMENTAL DATA
FEMALE GENITALS
GLANDS
HORMONES
INFORMATION
LABELLED COMPOUNDS
MAMMALS
MAMMARY GLANDS
NEOPLASMS
NUMERICAL DATA
ORGANS
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
STEROID HORMONES
TISSUE DISTRIBUTION
TRITIUM COMPOUNDS
UTERUS
VERTEBRATES