(I-125) 17. cap alpha. -Iodovinyl 11. beta. -methoxyestradiol: in vivo and in vitro properties of a high-affinity estrogen-receptor radiopharmaceutical
17 ..cap alpha..-(/sup 125/I)Iodovinyl 11 ..beta..-methoxyestradiol ((I-125)MIVE/sub 2/) has been prepared with high specific activity (155-2000 Ci/mmol) and a high affinity for the estrogen receptor. In vivo distribution studies using immature rats result in high levels of activity in the uterus (20-30% dose/g) with uterus-to-plasma ratios on the order of 68 to 100. Peak activity in the uterus is obtained between 2 and 4 hr, and by 6 hr 50% of the activity has washed out. The radioactive labeling of MIVE/sub 2/ is sufficiently rapid so that (I-123)MIVE/sub 2/ has been synthesized and is currently in clinical trials. These results suggest that MIVE/sub 2/ would be an excellent agent for the study of estrogen receptors in vivo and in vitro.
- Research Organization:
- Georgetown Univ., Washington, DC
- OSTI ID:
- 7056031
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:4
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ESTROGENS
RECEPTORS
TISSUE DISTRIBUTION
IODINE 125
RADIOPHARMACEUTICALS
CHEMICAL PROPERTIES
IN VITRO
IN VIVO
RATS
UTERUS
ANIMALS
BETA DECAY RADIOISOTOPES
BODY
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
FEMALE GENITALS
HORMONES
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPES
RODENTS
STEROID HORMONES
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
550501 - Metabolism- Tracer Techniques