RADIOLABELING AND BIODISTRIBUTION OF AMIODARONE AND DESETHYLAMIODARONE

被引:8
作者
BELLEN, JC [1 ]
PENGLIS, S [1 ]
TSOPELAS, C [1 ]
机构
[1] ROYAL ADELAIDE HOSP,DEPT NUCL MED,RADIOPHARM SECT,ADELAIDE,SA 5000,AUSTRALIA
来源
NUCLEAR MEDICINE AND BIOLOGY | 1995年 / 22卷 / 07期
关键词
D O I
10.1016/0969-8051(95)94367-M
中图分类号
R8 [特种医学]; R445 [影像诊断学];
学科分类号
1002 ; 100207 ; 1009 ;
摘要
The antiarrhythmic drug amiodarone and its metabolite desethylamiodarone, were radiolabeled with sodium [I-123]-iodide in >98% yield using the exchange labeling method. Biodistribution studies with I-123-amiodarone in mice showed high liver and lung uptake. Heart uptake of 0.98% of the injected dose (id) peaked at 5 min, with clearance seen over 60 min to 0.44% id. I-123-Desethylamiodarone (I-123-DEA) showed heart uptake of 0.58% id peaking at 5 min, with slower clearance seen over 60 min to 0.43% id. These results indicate that both agents have poor selectivity as myocardial imaging tracers. Low I-123-DEA brain uptake at 5 min (0.49% id) and rapid washout after 60 min indicate that I-123-desethylamiodarone has limited application as a brain imaging agent.
引用
收藏
页码:953 / 955
页数:3
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