Analogues of estradiol as potential breast tumor imaging agents
The radioiodinated analogue of estradiol, 11..beta..-methoxy-17..cap alpha..-(/sup 125/I)iodovinylestradiol (MIVE/sub 2/), has been shown to be a good candidate for the imaging of estrogen dependent breast tumors. Although there has been no extensive study on the sensitivity of radiotracers of this type, the authors have not observed localization of the radiotracer in metastatic lesions containing less than 20 fmole estrogen receptor/mg protein or in bone metasteses. In order to improve the sensitivity, they have examined several structural analogues of moxestrol (the parent structure for MIVE/sub 2/) for affinity to the ER isolated from immature rat uterus. The 11..beta..-ethyl analogue (EEE/sub 2/) of ethynyl estradiol (EE/sub 2/) exhibits the highest affinity with the 11..beta..-methyl analogue second best. Although the lipophilicity is also very high this compound should not be much more lipophilic than 16-iodoestradiol or MIVE/sub 2/ since the introduction of iodine increases the log P by greater than 1. The distribution of the tritiated derivative of EEE/sub 2/ is under study.
- Research Organization:
- Radiopharmaceutical/Medicinal Chemistry, The George Washington Univ. Medical Center, Washington, DC 20037
- OSTI ID:
- 6932823
- Report Number(s):
- CONF-840619-; TRN: 87-008856
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:5; Conference: 31. annual meeting of the Society of Nuclear Medicine, Los Angeles, CA, USA, 5 Jun 1984
- Country of Publication:
- United States
- Language:
- English
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ESTRADIOL
DIAGNOSTIC USES
STRUCTURE-ACTIVITY RELATIONSHIPS
TRACER TECHNIQUES
MAMMARY GLANDS
NEOPLASMS
METASTASES
DIAGNOSIS
AFFINITY
IMAGE PROCESSING
IODINE 125
ORGANIC IODINE COMPOUNDS
PROTEINS
RATS
RECEPTORS
SENSITIVITY
SKELETON
UTERUS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
DAYS LIVING RADIOISOTOPES
DISEASES
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
ESTROGENS
FEMALE GENITALS
GLANDS
HORMONES
HYDROXY COMPOUNDS
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
MEMBRANE PROTEINS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANS
PROCESSING
RADIOISOTOPES
RODENTS
STEROID HORMONES
STEROIDS
USES
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics