Fluorine-18 labeled 11β-substituted estrogens: Synthesis, receptor binding, and comparative target tissue uptake studies
✍ Scribed by M. G. Pomper; A. Katzenellenbogen; R. D. Thomas; C. J. Mathias; H. van Brocklin; M. J. Welch
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 152 KB
- Volume
- 26
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
Estrogens labeled with fluorine-I 8 show selective receptor-mediated uptake into estrogen target tissues,' and one agent, 1 6u-[1~F]fluoroestradiol ( l ) , has been used to image estrogen receptor-positive human breast tumors.2 In order to improve on the uptake characteristics of 1, we have examined the effect of 11 p-ethyl and 11 p-methoxy groups, as substituents at this site are known to substantially affect the binding behavior of estr0gens.3~4 The llp-methoxy substituent has been used by us5 and others6-8 to improve the target tissue uptake selectivity of estrogens labeled with the gamma emitters Br-77 and 1-125.