16 beta-[18F]fluoromoxestrol: a potent, metabolically stable positron emission tomography imaging agent for estrogen receptor positive human breast tumors.

Abstract

16 beta-[18F]Fluoromoxestrol (beta FMOX, 1) is a highly selective, metabolically stable estrogen with potential as a receptor imaging agent. It demonstrates receptor-mediated uptake in the immature rat in the estrogen receptor-rich primary target tissues, uterus and ovaries, as well as, in receptor-poor secondary target tissues, muscle, thymus and kidneys; uptake in the uterus is nearly four times that of the clinically useful 16 alpha-[18F]fluoroestradiol (FES), most likely due to the extended lifetime of the labeled beta FMOX in the blood afforded by its relatively slow metabolism. In vivo and in vitro studies demonstrate a nearly four-fold decrease in metabolism rate between beta FMOX and FES. Dosimetry studies indicate radiation absorbed doses comparable to FES. beta FMOX possesses desirable imaging characteristics and may prove to be a clinically useful imaging agent.

• Authors: H F VanBrocklin, P A Rocque, H V Lee, K E Carlson, J A Katzenellenbogen, M J Welch
• Journal: Life sciences (Life Sci) Vol. 53 Issue 10 Pg. 811-9 ( 1993) ISSN: 0024-3205 [Print] Netherlands
• PMID: 8355567 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Fluorine Radioisotopes
• Receptors, Estrogen
• fluoromoxestrol
• Ethinyl Estradiol

Topics

• Animals
• Breast Neoplasms (diagnostic imaging, ultrastructure)
• Ethinyl Estradiol (analogs & derivatives)
• Female
• Fluorine Radioisotopes
• Humans
• Liver (cytology, metabolism)
• Rats
• Rats, Sprague-Dawley
• Receptors, Estrogen (analysis)
• Tomography, Emission-Computed