Synthesis and biological evaluation of a fluorine-18 labeled estrogen receptor-alpha selective ligand: [18F] propyl pyrazole triol.
The two estrogen receptor subtypes, ERalpha and ERbeta, play important roles in breast cancer. To develop an ERalpha imaging agent, we synthesized fluoropropyl pyrazole triol (FPPT, 2), an analog of our ERalpha-selective ligand PPT. FPPT retains the high ERalpha binding selectivity of its parent PPT. We prepared [(18)F]FPPT ((18)F-2) in high specific activity, but estrogen target tissue uptake in female rats was minimal and was not displaceable by unlabeled estradiol, probably because of the lipophilicity and triphenolic nature of FPPT.
Vijaykumar
Dange
D
Department of Chemistry, University of Illinois, 600 S. Mathews Avenue, Urbana, Illinois 61801, USA.
Al-Qahtani
Mohammed H
MH
Welch
Michael J
MJ
Katzenellenbogen
John A
JA
D000818:Animals; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005260:Female; D005462:Fluorine Radioisotopes; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D051381:Rats; D011960:Receptors, Estrogen / Q000378:metabolism; D014018:Tissue Distribution
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D005462:Fluorine Radioisotopes; D011720:Pyrazoles; D019275:Radiopharmaceuticals; D011960:Receptors, Estrogen; C031280:pyrazole