Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2154918 | Nuclear Medicine and Biology | 2006 | 5 Pages |
Abstract
The endothelin-A receptor ligand Atrasentan (ABT-627) was radiolabeled by 11C-methylaton of the desmethyl precursor in phenolate form. In mice, the highest uptake of [11C]ABT-627 was in the liver, kidneys and lungs. No significant binding was observed in mouse brain or heart. PET studies in a baboon, however, showed accumulation in the myocardium and lungs with a tissue/blood equilibrium reached at 40 min postinjection. Between 35 and 75 min, the heart/blood and lung/blood ratios were 1.72 and 1.31, respectively. Pretreatment with a 0.39 mg/kg dose of unlabeled ABT-627 inhibited the uptake of the tracer by 53–54% in both the myocardium and lungs at 65 min.
Keywords
Related Topics
Life Sciences
Biochemistry, Genetics and Molecular Biology
Cancer Research
Authors
William B. Mathews, Tamas G. Zober, Hayden T. Ravert, Ursula Scheffel, John Hilton, Darryl Sleep, Robert F. Dannals, Zsolt Szabo,