Compartmental modeling of 11C-HOMADAM binding to the serotonin transporter in the healthy human brain.
Compartmental modeling of 11C-HOMADAM binding to the serotonin transporter in the healthy human brain.
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DOI：
10.2967/jnumed.108.054262
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发表时间：
2008-12
期刊：
影响因子：
--
通讯作者：
Goodman MM
中科院分区：
文献类型：
--
作者：
Nye JA;Votaw JR;Jarkas N;Purselle D;Camp V;Bremner JD;Kilts CD;Nemeroff CB;Goodman MM
新型 PET 放射性配体 11C-N,N-二甲基-2-(2'-氨基-4'-羟甲基苯硫基)苄胺 (11C-HOMADAM) 以高亲和力选择性地与血清素转运蛋白 (SERT) 结合。本研究的目的是开发一个可靠的动力学模型来描述健康人脑中 11C-HOMADAM 的摄取。八名志愿者参与了这项研究；其中 5 人安装了用于采血的动脉导管，并在注射 11C-HOMADAM 后使用高分辨率研究断层扫描仪进行扫描。使用 2 参数和 4 参数动脉输入室模型、3 参数参考组织室模型和 Logan 图形方法计算区域分布体积和结合电位。 2 参数动脉输入室模型在统计上优于 4 参数模型，并且描述了所有大脑区域。当小脑用作参考组织时，计算出的结合电位在动脉输入模型和参考组织模型之间非常一致。 Logan 图法无法估计中缝背侧 SERT 浓度高于中脑。 11C-HOMADAM 是一种非常有前途的放射性配体，在已知的富含 SERT 的结构（例如中缝核）中具有高特异性结合与非特异性结合的比率。 3 参数参考组织模型方法允许采用简化的定量准确方法来估计 SERT 结合电位。
The novel PET radioligand 11C-N,N-dimethyl-2-(2′-amino-4′-hydroxymethylphenylthio)benzylamine (11C-HOMADAM) binds with high affinity and selectively to the serotonin transporter (SERT). The purpose of this study was to develop a reliable kinetic model to describe the uptake of 11C-HOMADAM in the healthy human brain. Eight volunteers participated in the study; 5 of them were fitted with arterial catheters for blood sampling and all were scanned on a high-resolution research tomograph after the injection of 11C-HOMADAM. Regional distribution volumes and binding potentials were calculated with 2- and 4-parameter arterial-input compartment models, a 3-parameter reference tissue compartment model, and the Logan graphic approach. The 2-parameter arterial-input compartment model was statistically superior to the 4-parameter model and described all brain regions. Calculated binding potentials agreed well between the arterial-input model and the reference tissue model when the cerebellum was used as the reference tissue. The Logan graphic approach was not able to estimate the higher concentration of SERT in the dorsal raphe than in the midbrain. 11C-HOMADAM is a highly promising radioligand with high ratios of specific binding to nonspecific binding in known SERT-rich structures, such as the raphe nuclei. The 3-parameter reference tissue model approach permits a simplified quantitatively accurate method for estimating SERT binding potentials.
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影响因子：
2.9
作者：
BACKSTROM, I;BERGSTROM, M;MARCUSSON, J
通讯作者：
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影响因子：
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作者：
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5
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通讯作者：
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作者：
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