title: Synthesis and biodistribution of [125I]iodo- and [75Se]seleno-ergoline derivatives.
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.
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D016566:Organoselenium Compounds; D010479:Pergolide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism; D011868:Radioisotopes; D051381:Rats; D011919:Rats, Inbred Strains; D012643:Selenium; D014018:Tissue Distribution
chemical_list: D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D016566:Organoselenium Compounds; D011868:Radioisotopes; C052957:selenopergolide; C052958:8-iodomethyl-6-propylergoline; D010479:Pergolide; D012643:Selenium