RETARDATION OF 17-OXIDATION OF 160-ALPHA-[F-18]FLUOROESTRADIOL-17-BETA BY SUBSTITUTION OF DEUTERIUM FOR HYDROGEN IN THE 17-ALPHA POSITION(6)

Authors
BONASERA TA JONSON SD PAJEAU TS KATZENELLENBOGEN JA WELCH MJ
Citation
Ta. Bonasera et al., RETARDATION OF 17-OXIDATION OF 160-ALPHA-[F-18]FLUOROESTRADIOL-17-BETA BY SUBSTITUTION OF DEUTERIUM FOR HYDROGEN IN THE 17-ALPHA POSITION(6), Nuclear medicine and biology, 24(3), 1997, pp. 239-249
Citations number
46
Categorie Soggetti
Radiology,Nuclear Medicine & Medical Imaging
Journal title
Nuclear medicine and biology
ISSN journal
09698051 → ACNP
Volume
24
Issue
3
Year of publication
1997
Pages
239 - 249
Database
ISI
SICI code
0969-8051(1997)24:3<239:RO1O1>2.0.ZU;2-S
Abstract
We describe the synthesis, in vitro metabolism and biodistribution of [17 alpha-H-2]16 alpha-[F-18]fluoroestradiol ([F-18]DFES). The clinica lly useful breast cancer imaging agent, 16 alpha-[F-18]fluoroestradiol -17 beta ([F-18]FES), was deuterated at the C-17 alpha position to low er the rate of C-17 alcohol oxidation, Metabolism studies in immature female rat and mature female baboon isolated hepatocytes showed [F-18] DFES being consumed ca. 2.5 times slower than [F-18]FES. Biodistributi on studies and time activity curve measurements in female rats showed [F-18]DFES to have superior uptake characteristics compared to [F-18]F ES for imaging estrogen-receptor rich targets. (C) 1997 Elsevier Scien ce Inc.