Radiolabeled androgens and progestins as imaging agents for tumors of the prostate and breast. Technical progress report, February 1, 1992--January 31, 1993

Technical Report · Sat Aug 08 00:00:00 EDT 1992

DOI:https://doi.org/10.2172/10110956· OSTI ID:10110956

Katzenellenbogen, J A

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, Washington, DC (United States)
• DOE Contract Number: FG02-86ER60401
• OSTI ID: 10110956
• Report Number(s): DOE/ER/60401-3; ON: DE93006145
• Resource Relation: Other Information: PBD: 8 Aug 1992
• Country of Publication: United States
• Language: English

Related Subjects

62 RADIOLOGY AND NUCLEAR MEDICINE
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
ANDROGENS
LABELLING
ESTROGENS
PROGRESS REPORT
PROSTATE
MAMMARY GLANDS
TECHNETIUM 99
RHENIUM 186
RADIOPHARMACEUTICALS
POSITRON COMPUTED TOMOGRAPHY
PROGESTERONE
FLUORINE 18
TISSUE DISTRIBUTION
RECEPTORS
550601
400700
UNSEALED RADIONUCLIDES IN DIAGNOSTICS
RADIOCHEMISTRY AND NUCLEAR CHEMISTRY