Preparation of four fluorine-18-labeled estrogens and their selective uptakes in target tissues of immature rats

Journal Article · Thu Nov 01 04:00:00 EST 1984 · J. Nucl. Med.; (United States)

OSTI ID:6153619

Kiesewetter, D O; Kilbourn, M R; Landvatter, S W; Heiman, D F; Katzenellenbogen, J A; Welch, M J

Four fluorine-18-labeled estrogens have been prepared by simple displacement reactions utilizing reactive trifluoromethane sulfonate (triflate) precursors and F-18 fluoride ion. All four fluoroestrogens have high affinity for the estrogen receptor. In immature female rats, they are taken up by target tissues, such as the uterus, with very high selectivity: uterus-to-blood ratios at 1 hr are: Compound 1, 39; Compound 2, 12; Compound 3, 13; and Compound 4, 19. That the uptake process involves an estrogen-specific binder of limited capacity is demonstrated by the suppressive effect of coadministered unlabeled estradiol on target tissue uptake.

• Research Organization: Univ. of Illinois, Urbana
• DOE Contract Number: FG02-84ER60218
• OSTI ID: 6153619
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:11; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CHEMICAL PREPARATION
DATA
DISTRIBUTION
DRUGS
ESTROGENS
EXPERIMENTAL DATA
FEMALE GENITALS
FLUORIDES
FLUORINE 18
FLUORINE COMPOUNDS
FLUORINE ISOTOPES
HALIDES
HALOGEN COMPOUNDS
HORMONES
HOURS LIVING RADIOISOTOPES
INFORMATION
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MAMMALS
NUCLEI
NUMERICAL DATA
ODD-ODD NUCLEI
ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
STEROID HORMONES
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
UTERUS
VERTEBRATES