Radiolabeled androgens and progestins as imaging agents for tumors of the prostate and breast
We are preparing progestins and androgens, labeled with the single photon emitters technetium-99m and rhenium-186 and the positron-emitting radionuclide fluorine-18. In both cases, ligands selected have very high affinity for the respective receptor, low affinity for blood and non-specific binders and to be reasonably resistant to metabolism: The progestins will be derivatives of the potent progestins ORG2058, norgestrel, RU486, and an unusual retroprogestin and the androgens will be derivatives of the high affinity analogs of natural and synthetic androgens. Radiometal labeling will involve carefully designed steroid conjugates with N[sub 2]S[sub 2] or related chelates, or novel metal linkages, and metal complexes that themselves mimic a steroid. Fluorine substitution will be made at positions where bulk and polarity are tolerated and metabolic defluorination is minimal. In vitro competitive binding studies will be performed on the unlabeled analogs to determine their binding characteristics towards a series of steroid receptors and blood binding proteins, and Log P values will be estimated from BPLC. Tissue distribution studies with the radiolabeled progestins will be done in estrogen-primed rats using the uterus as a target, and with the radioandrogens in estrogen-treated rats using the prostate as a target. Ultimately, in collaborative studies, these radiopharmaceuticals are to be used with SPECT or PET to image the receptor-positive tumors.
- Research Organization:
- Univ. of Illinois at Urbana-Champaign, IL (United States)
- Sponsoring Organization:
- USDOE; USDOE, Washington, DC (United States)
- DOE Contract Number:
- FG02-86ER60401
- OSTI ID:
- 6853675
- Report Number(s):
- DOE/ER/60401-3; ON: DE93006145
- Country of Publication:
- United States
- Language:
- English
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(Fluorine-18 labeled androgens and progestins: Imaging agents for tumors of the prostate and breast)
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38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
ANDROGENS
LABELLING
ESTROGENS
FLUORINE 18
MAMMARY GLANDS
POSITRON COMPUTED TOMOGRAPHY
PROGESTERONE
PROGRESS REPORT
PROSTATE
RADIOPHARMACEUTICALS
RECEPTORS
RHENIUM 186
TECHNETIUM 99
TISSUE DISTRIBUTION
ANDROSTANES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
COMPUTERIZED TOMOGRAPHY
DAYS LIVING RADIOISOTOPES
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DOCUMENT TYPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EMISSION COMPUTED TOMOGRAPHY
FLUORINE ISOTOPES
GLANDS
HEAVY NUCLEI
HORMONES
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
KETONES
LABELLED COMPOUNDS
LIGHT NUCLEI
MALE GENITALS
MEMBRANE PROTEINS
NANOSEC LIVING RADIOISOTOPES
NUCLEI
ODD-EVEN NUCLEI
ODD-ODD NUCLEI
ORGANIC COMPOUNDS
ORGANS
PREGNANES
PROTEINS
RADIOISOTOPES
RHENIUM ISOTOPES
STEROID HORMONES
STEROIDS
TECHNETIUM ISOTOPES
TOMOGRAPHY
YEARS LIVING RADIOI
YEARS LIVING RADIOISOTOPES
550601* - Medicine- Unsealed Radionuclides in Diagnostics
400700 - Radiochemistry & Nuclear Chemistry