New selenium-75 labeled radiopharmaceuticals: selenonium analogs of dopamine

Selenium-75 labeled selenonium analogues of dopamine, [2-(3,4-dimethoxyphenyl)ethyl]dimethylselenonium iodide (4) and its dihydroxy analogue (7), were prepared by reducing [75Se]selenious acid with sodium borohydride at pH 6.0 and reacting the NaSeH produced with 1-(3,4-dimethoxyphenyl)-2-(p-toluene...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1983-07, Vol.26 (7), p.947-950
Main Authors: Sadek, Samy A, Basmadjian, Garo P, Hsu, Pan M, Rieger, Joseph A
Format: Article
Language:English
Subjects:
Adrenal Glands - metabolism
Animals
Brain - metabolism
Dopamine - analogs & derivatives
Dopamine - chemical synthesis
Dopamine - metabolism
Female
Kidney - metabolism
Kinetics
Liver - metabolism
Lung - metabolism
Myocardium - metabolism
Organoselenium Compounds
Radioisotopes
Rats
Rats, Inbred Strains
Selenium - chemical synthesis
Selenium - metabolism
Structure-Activity Relationship
Tissue Distribution
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Summary:Selenium-75 labeled selenonium analogues of dopamine, [2-(3,4-dimethoxyphenyl)ethyl]dimethylselenonium iodide (4) and its dihydroxy analogue (7), were prepared by reducing [75Se]selenious acid with sodium borohydride at pH 6.0 and reacting the NaSeH produced with 1-(3,4-dimethoxyphenyl)-2-(p-toluenesulfonyloxy)ethane. Tissue distribution studies in rats given the 75Se-labeled selenonium agents intravenously demonstrated high initial heart uptake (2.38% dose/g at 5 min). Prolonged adrenal retention (t1/2 = 10 h) and high adrenal to blood ratio of compound 4 (21/1 at 4 h after injection) were observed. The high uptake and adrenal to blood ratio suggest the potential use of compound 4 as a radiopharmaceutical for the adrenal gland.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00361a003