Characterization of high specific activity (16 alpha-123I)Iodo-17 beta-estradiol as an estrogen receptor-specific radioligand capable of imaging estrogen receptor-positive tumors
- Univ. of Kentucky College of Medicine, Lexington (USA)
16 alpha-(123I)Iodo-17 beta-estradiol (16 alpha-(123I)E2) has been characterized for use as a selective radioligand for estrogen receptor (ERc) that is capable of generating in situ images of ERc-positive tumors. High specific activity 16 alpha-(123I)E2 (7,500-10,000 Ci/mmol) was used in all determinations. Radiochemical purity was determined by thin layer chromatography, and the selectivity of radioligand for ERc was evaluated using size exclusion high performance liquid chromatography on ERc prepared from rodent uteri. Efficiencies of radioidination approaching 100% were achieved, and excellent receptor selectivity was obtained even when the efficiency of radioiodination was as low as 10%. Low radiochemical purity was always associated with poor selectivity for ERc. No new radioligand species was generated during the course of radiodecay; however, reduced binding over time, even when increased activity was used to compensate for radiodecay, indicated that the formation of a radioinert competitor does occur. 16 alpha-(123I)E2 demonstrated stable, high affinity binding to ERc and was concentrated by ERc-positive tissues. After injecting 16 alpha-(123I)E2 in vivo, images of ERc-containing tissues were obtained, including rabbit reproductive tract and dimethylbenzanthracene-induced tumors. The demonstrations of ERc selectivity and image formation both indicate that 16 alpha-(123I)E2 should have promise as a useful new radiopharmaceutical for imaging ERc-positive cancers.
- OSTI ID:
- 6273302
- Journal Information:
- Cancer Research; (USA), Vol. 50:24; ISSN 0008-5472
- Country of Publication:
- United States
- Language:
- English
Similar Records
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]
Comparison of immunocytochemical estrogen receptor assay, estrogen receptor enzyme immunoassay, and radioligand-labeled estrogen receptor assay in human breast cancer and uterine tissue
Related Subjects
ESTROGENS
RECEPTORS
EXPERIMENTAL NEOPLASMS
DIAGNOSIS
RADIOPHARMACEUTICALS
CHEMICAL COMPOSITION
UTERUS
BIOCHEMICAL REACTION KINETICS
ESTRADIOL
IMAGE PROCESSING
IODINE 123
LIGANDS
LIQUID COLUMN CHROMATOGRAPHY
MICE
RABBITS
RATS
THIN-LAYER CHROMATOGRAPHY
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
CHROMATOGRAPHY
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
FEMALE GENITALS
HORMONES
HOURS LIVING RADIOISOTOPES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
PROCESSING
PROTEINS
RADIOISOTOPES
REACTION KINETICS
RODENTS
SEPARATION PROCESSES
STEROID HORMONES
STEROIDS
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics