7alpha- and 17alpha-substituted estrogens containing tridentate tricarbonyl rhenium/technetium complexes: synthesis of estrogen receptor imaging agents and evaluation using microPET with technetium-94m.
To develop technetium and rhenium-labeled imaging agents for estrogen receptor (ER) positive breast tumors, we have prepared tridentate metal tricarbonyl chelates substituted at the 7alpha- and 17alpha-positions of estradiol. Some of the Re(CO)(3) conjugates have high binding for the ER in vitro. The in vivo biodistribution of the highest affinity of these novel metal tricarbonyl conjugates, prepared as the (94m)Tc labeled analogue, was evaluated by tissue dissection and microPET imaging. Although target tissue-selective uptake was not apparent, it is notable that microPET imaging identified the stomach as a major site of activity deposition, a site that might have been missed by standard tissue distribution studies.
Luyt
Leonard G
LG
Department of Chemistry, University of Illinois, 600 South Mathews Avenue, Urbana, IL 61801, USA.
Bigott
Heather M
HM
Welch
Michael J
MJ
Katzenellenbogen
John A
JA
D000818:Animals; D004967:Estrogens / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015609:Organotechnetium Compounds / Q000737:chemistry*; D019275:Radiopharmaceuticals / Q000737:chemistry*; D051381:Rats; D012211:Rhenium / Q000737:chemistry*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed / Q000379:methods*
D004967:Estrogens; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D012211:Rhenium