E-17 alpha(/sup 125/I)iodovinylestradiol: an estrogen-receptor-seeking radiopharmaceutical

Journal Article · Sat May 01 04:00:00 EDT 1982 · J. Nucl. Med.; (United States)

OSTI ID:6879760

Hanson, R N; Seitz, D E; Botarro, J C

Through the use of radioiododestannylation, the specifically labeled E-17 alpha-(/sup 125/I)iodovinylestradiol ((/sup 125/I)VE2) was synthesized rapidly and in high yield from the stable precursor E-17 alpha-tributylstannylvinylestradiol (SnVE2), and its biodistribution was determined in immature female rats. The agent accumulated in the uterus, achieving a peak uptake of 0.465% ID-kg/g at 2 hr. Uterus-to-blood ratios of 19 and 16 occurred at 1 and 2 hr, respectively, declining to 7 by 4 hr after injection. The uptake of (/sup 125/I)VE2 by the uterus at 2 hr was reduced 58--65% by pretreatment of the immature rats with estradiol (5 micrograms) or tamoxifen (100 micrograms), and compared with 16 alpha-(/sup 125/I)iodoestradiol, (/sup 125/I)VE2 showed greater uterine uptake and similar uterus-to-blood ratios. The ease of preparation of the radioligand represents an advantage over the synthetic procedures for other estrogen-receptor-seeking agents.

• Research Organization: Northeastern University, Boston, Massachusetts
• OSTI ID: 6879760
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 23:5; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702 -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601* -- Medicine-- Unsealed Radionuclides in Diagnostics
551001 -- Physiological Systems-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMISTRY
BIOLOGICAL LOCALIZATION
BODY
CHEMICAL PREPARATION
CHEMISTRY
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC USES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRANES
ESTROGENS
FEMALE GENITALS
HORMONES
INTERMEDIATE MASS NUCLEI
IODINE 125
IODINE ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANS
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RECEPTORS
RODENTS
STEROID HORMONES
STEROIDS
SYNTHESIS
TISSUE DISTRIBUTION
UPTAKE
USES
UTERUS
VERTEBRATES