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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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

(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.[1]

References

  1. Synthesis and biodistribution of [125I]iodo- and [75Se]seleno-ergoline derivatives. Sadek, S., Basmadjian, G., Patel, A. International journal of radiation applications and instrumentation. Part A, Applied radiation and isotopes. (1987) [Pubmed]
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