Fluorine-18-labeled estrogens, progestins and corticosteroids for receptor-based imaging of breast tumors and target areas of the brain

Estrogens can be labeled with the positron-emitting radionuclide fluorine-18 (t$\sb{1/2}$ = 110 min) by fluoride ion (n-Bu$\sb4$N$\sp{18}$F) displacement of a 16β-trifluoromethanesulfonate (triflate) derivative of the corresponding estrone 3-triflate, and purification by HPLC. That sequence has been used to synthesize the 11β-methoxy 1 and 11β-ethyl 2 analogues of the breast tumor imaging agent, 16α-($\sp{18}$F) fluoro-17β-estradiol (FES). Tissue distribution studies of 1 and 2 in immature female rats show high selectivity for target tissue (T, uterus) vs non-target (NT, muscle and lung), with T/NT ratios being 43 and 17 at one hour after injection for 1 and 2, respectively. The parent estrogen FES has previously been shown to display an intermediate value for tissue selectivity.

Name thesis:degree_name

Ph.D.

Level thesis:degree_level

Dissertation

Discipline thesis:degree_discipline

Chemistry

Grantor

University of Illinois at Urbana-Champaign

Year dc:date

2011

Author dc:creator

• Pomper, Martin Gilbert

• Organic Chemistry
• Pharmaceutical Chemistry
• Health Sciences
• Radiology

Statement dc:rights

• Copyright 1989 Pomper, Martin Gilbert

Language dc:language

eng

Identifier

AAI9010990
(UMI)AAI9010990

OAI identifier oai:identifier

oai:www.ideals.illinois.edu:2142/19008