Bromine-80m-labeled estrogens: Auger-electron emitting, estrogen receptor-directed ligands with potential for therapy of estrogen receptor positive cancers
A triphenylbromoethylene, 1,1-bis(p-hydroxyphenyl)-2-bromo-2-phenylethylene, Br-BHPE, and a bromosteroidal estrogen, 17..cap alpha..- bromovinylestradiol, BrVE/sub 2/, were labeled with the Auger electron emitting nuclide bromine-80m, prepared by the (p,n) reaction with /sup 80/Se. To assess their potential as estrogen receptor (ER) directed therapeutic substrates the bromine-80m labeled estrogens were injected into immature female rats and the tissue distribution studied at 0.5 and 2 hours. Both radiobromoestrogens showed substantial diethylstilbesterol (DES)-inhibitable localization in the ER rich tissues, uterus, pituitary, ovary and vagina at both time points. While the percent dose per gram tissue was higher for the Br-BHPE, the BrVE/sub 2/ showed higher tissue to blood ratios, especially at 2 hr, reflecting the lower blood concentrations of radiobromine following administration of the steroidal bromoestrogen. Comparing intraperitoneal, intravenous and subcutaneous routes of administration for the radiobromine labeled Br-BHPE, the intraperitoneal route was particularly advantageous to provide maximum, DES-inhibitable concentrations in the peritoneal, ER-rich target organs, the uterus, ovary and vagina. While uterine concentrations after BrBHPE were from 10--48% dose/g and after BrVE/sub 2/ were 15--25% dose/g, similar treatment with /sup 80m/Br as sodium bromide showed uniform low concentrations in all tissues at about the levels seen in blood. The effective specific activity of (/sup 80m/Br)BrBHPE, assayed by specific binding to ER in rat uterine cytosol, was 8700 Ci/mmole. 23 refs., 9 figs., 2 tabs.
- Research Organization:
- Argonne National Lab. (ANL), Argonne, IL (United States)
- DOE Contract Number:
- W-31109-ENG-38
- OSTI ID:
- 6347502
- Report Number(s):
- ANL/PPRNT-89-172; ON: DE89008478
- Resource Relation:
- Other Information: Portions of this document are illegible in microfiche products
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
BROMINE 80
RADIONUCLIDE KINETICS
NEOPLASMS
RADIOTHERAPY
AUGER EFFECT
ESTROGENS
HOT ATOM CHEMISTRY
ISOTOPE EFFECTS
LABELLING
ORGANIC BROMINE COMPOUNDS
RADIOPHARMACEUTICALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BROMINE ISOTOPES
CHEMISTRY
DISEASES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HORMONES
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MEDICINE
MINUTES LIVING RADIOISOTOPES
NUCLEAR MEDICINE
NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
RADIOCHEMISTRY
RADIOISOTOPES
RADIOLOGY
STEROID HORMONES
THERAPY
550604* - Medicine- Unsealed Radionuclides in Therapy- (1980-)