Preparation and evaluation of 17. cap alpha. -(/sup 125/I)iodovinyl-11. beta. -methoxyestradiol as a highly selective radioligand for tissues containing estrogen receptors: concise communication. [Rats]
The moxestrol analog 17..cap alpha..-(/sup 125/I)iodovinyl-11..beta..-methoxyestradiol was prepared in 95% radiochemical yield from the corresponding 17..cap alpha..-(tributylstannyl)vinyl compound and no-carrier-added sodium (/sup 125/I)iodide. The new radioligand was evaluated in immature female rats to determine the uptake in and selectivity for tissues containing estrogen receptors. At 1, 2, and 6 hr after injection, the agent demonstrates both high selectivity (uterus to blood ratio) and a high concentration in the largest tissue. The compounds's biologic properties and its ease of preparation suggest that it would be a likely candidate for clinical use as an estrogen-receptor-seeking radiopharmaceutical.
- Research Organization:
- Northeastern Univ., Boston, MA
- DOE Contract Number:
- AC02-76EV04115
- OSTI ID:
- 6764926
- Journal Information:
- J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:9; ISSN JNMEA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
CHEMICAL PREPARATION
CHROMATOGRAPHY
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HORMONES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
LIVER
LUNGS
MAMMALS
MATERIALS
MUSCLES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RESPIRATORY SYSTEM
RODENTS
SEPARATION PROCESSES
STEROID HORMONES
STEROIDS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
UTERUS
VERTEBRATES