Biodistribution and metabolism of 16. cap alpha. -((/sup 18/F)-fluoro)-17. beta. -estradiol

Conference · Wed May 01 04:00:00 EDT 1985 · J. Nucl. Med.; (United States)

OSTI ID:6854667

Mathias, C J; Brodack, J W; Kilbourn, M R; Carlson, K A; Katzenellenbogen, J A; Welch, M J

The uptake of receptor-mediated radiopharmaceuticals as measured by target to non-target uptake ratios depends upon many parameters. These include blood flow to the tissue, blood volume, receptor concentration as well as metabolism of the tracer. In a rat tumor model (DMBA) induced mammary tumors with high concentration of estrogen receptors) uptake of /sup 18/F-estradiol was studied while blood flow was measured with the use of /sup 125/I-iodoantipyrine, blood volume was measured with the use of /sup 99m/Tc-labeled red blood cells, and the receptor concentration by in vitro assay. The results demonstrate no correlation between blood flow and uptake of ligand, or between receptor concentration and uptake of ligand. No correlation existed between blood volume and uptake or /sup 18/F-estradiol, even though the blood volume varied by a factor of --20 in the tumors studied. The distribution of the fluorine-18 may depend upon metabolites of the ligand rather than the ligand itself. The authors have developed a technique to separate metabolites from the administered compound in blood and tissues. The distribution of the compound in the blood at times >30 mins after injection was primarily within the red blood cells in a chemical form that was not extractable even in lysed blood samples. By injecting blood from one rate into another the authors have shown that the activity in blood 2 hours after injection of /sup 18/F-estradiol is not available for uptake in receptor rich tissue but remains in the blood and non-target tissues.

• Research Organization: The Edward Mallinckrodt Institute of Radiology, Washington Univ. School of Medicine, St. Louis, MO
• OSTI ID: 6854667
• Report Number(s): CONF-850611-
• Conference Information: Journal Name: J. Nucl. Med.; (United States) Journal Volume: 26:5
• Country of Publication: United States
• Language: English

Related Subjects

550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
AROMATICS
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BLOOD FLOW
COMPLEXES
CONDENSED AROMATICS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIAGNOSIS
DIAGNOSTIC USES
DIMETHYLBENZANTHRACENE
DISEASES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
EXTRACTION
FLUORINE 18
FLUORINE ISOTOPES
HORMONES
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
INJECTION
INTAKE
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE COMPLEXES
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
LIGANDS
LIGHT NUCLEI
MAMMALS
MEMBRANE PROTEINS
METABOLISM
NEOPLASMS
NUCLEI
ODD-EVEN NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
PROTEINS
RADIOISOTOPE SCANNING
RADIOISOTOPES
RADIONUCLIDE KINETICS
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
SEPARATION PROCESSES
STEROID HORMONES
STEROIDS
TISSUE DISTRIBUTION
UPTAKE
USES
VERTEBRATES