Synthesis and biodistribution of [125I]iodo- and [75Se]seleno-ergoline derivatives

Int J Rad Appl Instrum A. 1987;38(5):391-7. doi: 10.1016/0883-2889(87)90028-1.

Abstract

(8 beta)-8-([125]Iodomethyl)-6-propylergoline (125I-3) was prepared by refluxing the mesyl analog with Na125I in methyl-ethyl-ketone, followed by HPLC, in a radiochemical yield greater than 70%. [75Se]Selenopergolide (75Se-2) was prepared in 74% yield starting with H75(2) SeO3. The biodistribution studies of the two compounds in male rats show good uptake by the adrenals and the brain. Compound 75Se-2 had higher adrenal uptake and adrenal-to-blood ratios (4.2% dose/g and 70:1) than 125I-3 (3.6% dose/g and 23.8:1) at 15 min post injection. The two compounds had almost equal brain uptake (0.91% dose/g for 75Se-2 and 1.14% dose/g for 125I-3), but 75Se-2 showed higher brain-to-blood ratios (15.2:1 vs 7.3:1) at 15 min post injection. This study indicates that 75Se-2 and 123I-3 may be useful agents for imaging the adrenal and the brain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Indicators and Reagents
  • Iodine Radioisotopes*
  • Isotope Labeling / methods
  • Male
  • Organoselenium Compounds*
  • Pergolide / analogs & derivatives*
  • Pergolide / chemical synthesis
  • Pergolide / metabolism
  • Radioisotopes*
  • Rats
  • Rats, Inbred Strains
  • Selenium*
  • Tissue Distribution

Substances

  • Indicators and Reagents
  • Iodine Radioisotopes
  • Organoselenium Compounds
  • Radioisotopes
  • selenopergolide
  • 8-iodomethyl-6-propylergoline
  • Pergolide
  • Selenium