RECEPTOR-BINDING RADIOTRACERS FOR THE ANGIOTENSIN-II RECEPTOR - RADIOIODINATED [SAR(1),ILE(8)]ANGIOTENSIN-II

RECEPTOR-BINDING RADIOTRACERS FOR THE ANGIOTENSIN-II RECEPTOR - RADIOIODINATED [SAR(1),ILE(8)]ANGIOTENSIN-II
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DOI:
10.1016/0969-8051(94)90024-8
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发表时间:
1994-05-01
影响因子:
3.1
通讯作者:
BURNS, HD
BURNS, HD
中科院分区:
医学4区
文献类型:
--
作者:
GIBSON, RE;BEAUCHAMP, HT;BURNS, HD

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使用放射性碘化肽拮抗剂[I-125][Sar(1),Ile(8)]血管紧张素II评价血管紧张素II受体成像的潜力。放射性配体在大鼠的几种组织(肾脏、肾上腺和肝脏)中提供受体介导的信号。3% ID/g肾皮质的受体介导信号应足以允许成像,至少通过SPECT。放射性示踪剂对受体浓度的降低敏感,可用于确定血管紧张素II受体配体的体内剂量占用曲线。在大鼠肾脏和恒河猴肝脏中获得了[I-123][Sar(1),Ile(8)]血管紧张素II的受体介导图像。
The potential for imaging the angiotensin II receptor was evaluated using the radioiodinated peptide antagonist [I-125][Sar(1),Ile(8)]angiotensin II. The radioligand provides a receptor-mediated signal in several tissues in rat (kidneys, adrenal and liver). The receptor-mediated signal of 3% ID/g kidney cortex should be sufficient to permit imaging, at least via SPECT. The radiotracer is sensitive to reductions in receptor concentration and can be used to define in viva dose-occupancy curves of angiotensin II receptor ligands. Receptor-mediated images of [I-123][Sar(1),Ile(8)]angiotensin II were obtained in the rat kidney and Rhesus monkey liver.