Kauppinen Tomi A, Bergström Kim A, Heikman Pertti, Hiltunen Jukka, Ahonen Aapo K
Division of Nuclear Medicine, Helsinki University Central Hospital, P.O. Box 340, 00029 Helsinki, Finland.
Eur J Nucl Med Mol Imaging. 2003 Jan;30(1):132-6. doi: 10.1007/s00259-002-1027-7. Epub 2002 Nov 9.
[(123)I]ADAM [2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine (ADAM)] has recently been shown to be a very promising imaging ligand for the detection of serotonin transporters (SERT) in human brain, because of its high specificity for SERT. [(123)I]ADAM has previously been used only for animal studies. In this work, we investigated the radiation dosimetry and biodistribution of [(123)I]ADAM based on whole-body scans in healthy human volunteers. Following the administration of 196+/-20 MBq (range 157-220 MBq) [(123)I]ADAM, serial whole-body images were performed up to 24 h. Estimates of radiation absorbed dose were calculated using the MIRDOSE 3.0 program with a dynamic bladder model. Twelve source organs were considered in estimating absorbed radiation doses for organs of the body. The highest absorbed organ doses were found to the lower large intestine wall (8.3.10(-2) mGy/MBq), kidneys (5.2.10(-2) mGy/MBq), urinary bladder wall (4.9.10(-2) mGy/MBq) and thyroid (4.3.10(-2) mGy/MBq). The effective dose was estimated to be 2.2.10(-2) mSv/MBq. The results suggest that [(123)I]ADAM is of potential value as a tracer for single-photon emission tomography imaging of serotonin receptors in humans, with acceptable dosimetry and high brain uptake.
[(123)I]ADAM[2-((2-((二甲氨基)甲基)苯基)硫代)-5-碘苯胺(ADAM)]最近已被证明是一种非常有前景的用于检测人脑中5-羟色胺转运体(SERT)的成像配体,因为它对SERT具有高特异性。[(123)I]ADAM此前仅用于动物研究。在这项工作中,我们基于对健康人类志愿者的全身扫描研究了[(123)I]ADAM的辐射剂量学和生物分布。给予196±20MBq(范围157 - 220MBq)的[(123)I]ADAM后,进行长达24小时的系列全身图像采集。使用带有动态膀胱模型的MIRDOSE 3.0程序计算辐射吸收剂量估计值。在估计身体各器官的吸收辐射剂量时考虑了12个源器官。发现吸收器官剂量最高的是降大肠壁(8.3×10⁻²mGy/MBq)、肾脏(5.2×10⁻²mGy/MBq)、膀胱壁(4.9×10⁻²mGy/MBq)和甲状腺(4.3×10⁻²mGy/MBq)。有效剂量估计为2.2×10⁻²mSv/MBq。结果表明,[(123)I]ADAM作为人类5-羟色胺受体单光子发射断层成像的示踪剂具有潜在价值,其剂量学可接受且脑摄取率高。