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评估健康受试者和 1 型糖尿病患者中 [F]FP-DTBZ 的活性和非活性对映异构体与胰腺 VMAT2 的结合。

Evaluation of Pancreatic VMAT2 Binding with Active and Inactive Enantiomers of [F]FP-DTBZ in Healthy Subjects and Patients with Type 1 Diabetes.

机构信息

Yale University, P.O. Box 208048, New Haven, CT, 06520-8048, USA.

Columbia University, New York, NY, USA.

出版信息

Mol Imaging Biol. 2018 Oct;20(5):835-845. doi: 10.1007/s11307-018-1170-6.

DOI:10.1007/s11307-018-1170-6
PMID:29468404
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6533199/
Abstract

PURPOSE

Previous studies demonstrated the utility of [F]fluoropropyl-(+)-dihydrotetrabenazine ([F]FP-(+)-DTBZ) as a positron emission tomography (PET) radiotracer for the vesicular monoamine transporter type 2 (VMAT2) to quantify beta cell mass in healthy control (HC) and type 1 diabetes mellitus (T1DM) groups. Quantification of specific binding requires measurement of non-displaceable uptake. Our goal was to identify a reference tissue (renal cortex or spleen) to quantify pancreatic non-specific binding of [F]FP-(+)-DTBZ with the inactive enantiomer, [F]FP-(-)-DTBZ. This was the first human study of [F]FP-(-)-DTBZ.

PROCEDURES

Six HCs and four T1DM patients were scanned on separate days after injection of [F]FP-(+)-DTBZ or [F]FP-(-)-DTBZ. Distribution volumes (V) and standardized uptake values (SUVs) were compared between groups. Three methods for calculation of non-displaceable uptake (V) or reference SUV were applied: (1) use of [F]FP-(+)-DTBZ reference V as V, assuming V is uniform across organs; (2) use of [F]FP-(-)-DTBZ pancreatic V as V, assuming that V is uniform between enantiomers in the pancreas; and (3) use of a scaled [F]FP-(+)-DTBZ reference V as V, assuming that a ratio of non-displaceable uptake between organs is uniform between enantiomers. Group differences in V (or SUV), binding potential (BP), or SUV ratio (SUVR) were estimated using these three methods.

RESULTS

[F]FP-(-)-DTBZ V values were different among organs, and V(+) and V(-) were also different in the renal cortex and spleen. Method 3 with the spleen to estimate V (or reference SUV) gave the highest non-displaceable uptake and the largest HC vs. T1DM group differences. Significant group differences were also observed in V (or SUV) with method 1 using spleen. SUV was affected by differences in the input function between groups and between enantiomers.

CONCLUSIONS

Non-displaceable uptake was different among organs and between enantiomers. Use of scaled spleen V values for V is a suitable method for quantification of VMAT2 in the pancreas.

摘要

目的

先前的研究表明，[F]氟丙基-（+）-二氢四苯并嗪（[F]FP-（+）-DTBZ）作为正电子发射断层扫描（PET）示踪剂用于检测囊泡单胺转运体 2（VMAT2），以定量健康对照组（HC）和 1 型糖尿病（T1DM）组的β细胞量。特异性结合的定量需要测量不可置换的摄取。我们的目标是确定参考组织（肾皮质或脾脏）来量化[F]FP-（+）-DTBZ 与无活性对映体[F]FP-（-）-DTBZ 在胰腺中的非特异性结合。这是[F]FP-（-）-DTBZ 的首次人体研究。

过程

在注射[F]FP-（+）-DTBZ 或[F]FP-（-）-DTBZ 后，六名 HC 和四名 T1DM 患者在不同的日子进行扫描。比较组间分布容积（V）和标准化摄取值（SUV）。应用三种方法计算不可置换摄取（V）或参考 SUV：（1）使用[F]FP-（+）-DTBZ 参考 V 作为 V，假设 V 在器官之间均匀；（2）使用[F]FP-（-）-DTBZ 胰腺 V 作为 V，假设 V 在胰腺中两种对映体之间均匀；（3）使用比例[F]FP-（+）-DTBZ 参考 V 作为 V，假设器官之间非置换摄取的比值在两种对映体之间均匀。使用这三种方法估计 V（或 SUV）、结合潜力（BP）或 SUV 比值（SUVR）在组间的差异。

结果

[F]FP-（-）-DTBZ 的 V 值在器官之间不同，肾皮质和脾脏中的 V（+）和 V（-）也不同。使用脾脏估算 V（或参考 SUV）的方法 3 给出了最高的不可置换摄取和最大的 HC 与 T1DM 组间差异。使用脾脏的方法 1 也观察到 V（或 SUV）的显著组间差异。SUV 受到组间和两种对映体之间输入函数差异的影响。

结论

不可置换摄取在器官之间和两种对映体之间不同。使用比例脾脏 V 值进行 V 是定量胰腺 VMAT2 的合适方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/2d8472dcc9c5/nihms-997652-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/1e127410a807/nihms-997652-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/37070005d145/nihms-997652-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/0ce037c46bc0/nihms-997652-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/c3190fef3051/nihms-997652-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/2d8472dcc9c5/nihms-997652-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/1e127410a807/nihms-997652-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/37070005d145/nihms-997652-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/0ce037c46bc0/nihms-997652-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/c3190fef3051/nihms-997652-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aa9d/6533199/2d8472dcc9c5/nihms-997652-f0005.jpg

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