Radioiodinated ligands for the estrogen receptor: effect of 3-o-methylation on tissue distribution

Journal Article · Mon Oct 01 04:00:00 EDT 1984 · J. Nucl. Med.; (United States)

OSTI ID:6196052

Franke, L A; Hanson, R N

The 3-o-methyl ethers of 17..cap alpha..-(/sup 125/I)iodovinylestradiol and 17..cap alpha..(/sup 125/I)iodovinyl-11..beta..-methoxyestradiol were prepared in 95% and 89% isolated yields, respectively, at the no-carrier-added level from the corresponding (tri-n-butystannyl)-vinyl intermediates. The new radioligands were evaluated in immature female rats to determine their uptake in, and selectivity for, estrogen-receptor-containing tissues. At 0.5-6 hr after administration, both agents showed preferential uptake and retention by the target tissue. Compared with the parent 3-hydroxy radioligands, the (/sup 125/I)VE/sub 2/-3-o-Me had lower uptake and target-to-blood ratios at all time periods, but by 6 hr the (/sup 125/I)VME/sub 2/-3-o-Me compound showed as high an uptake in the uterus and higher uterus-to-blood ratios. The results suggest that iodine-123-labeled VME/sub 2/-3-o-Me would be a good candidate for in vivo gamma imaging of estrogen-containing tissues.

• Research Organization: Northeastern Univ., Boston, MA
• OSTI ID: 6196052
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:10; ISSN JNMEA
• Country of Publication: United States
• Language: English

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
ALKALI METAL COMPOUNDS
ANIMALS
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BODY
BODY FLUIDS
CHEMICAL PREPARATION
CHEMICAL REACTIONS
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTROGENS
FEMALE GENITALS
GLANDS
HALIDES
HALOGEN COMPOUNDS
HORMONES
INORGANIC PHOSPHORS
INTERMEDIATE MASS NUCLEI
IODIDES
IODINE 125
IODINE COMPOUNDS
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGANDS
LIVER
LUNGS
MAMMALS
MATERIALS
METHYLATION
MUSCLES
NUCLEI
ODD-EVEN NUCLEI
ORGANS
PHOSPHORS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RESPIRATORY SYSTEM
RODENTS
SODIUM COMPOUNDS
SODIUM IODIDES
STEROID HORMONES
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
UTERUS
VERTEBRATES