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First-in-Humans Brain PET Imaging of the GluN2B-Containing -methyl-d-aspartate Receptor with ()-C-Me-NB1.首次人体脑正电子发射断层扫描成像研究 GluN2B 包含型 -N- 甲基-D-天冬氨酸受体与 ()-C-Me-NB1。
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Metaplastic Effects of Ketamine and MK-801 on Glutamate Receptors Expression in Rat Medial Prefrontal Cortex and Hippocampus.氯胺酮和 MK-801 对大鼠前额叶皮质和海马谷氨酸受体表达的塑型作用。
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Preclinical Development of F-OF-NB1 for Imaging GluN2B-Containing -Methyl-d-Aspartate Receptors and Its Utility as a Biomarker for Amyotrophic Lateral Sclerosis.用于成像含 GluN2B 的 N-甲基-D-天冬氨酸受体的 F-OF-NB1 的临床前开发及其作为肌萎缩侧索硬化症生物标志物的效用。
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The ARRIVE guidelines 2.0: Updated guidelines for reporting animal research.《ARRIVE指南2.0：动物研究报告的更新指南》
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Synthesis and preliminary evaluation of novel C-labeled GluN2B-selective NMDA receptor negative allosteric modulators.新型 C 标记的 GluN2B 选择性 NMDA 受体负变构调节剂的合成与初步评价。
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A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists.一种全面描述 GluN2B 选择性 N-甲基-D-天冬氨酸（NMDA）受体拮抗剂的方法。
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Structure-Affinity Relationships of 2,3,4,5-Tetrahydro-1-3-benzazepine and 6,7,8,9-Tetrahydro-5-benzo[7]annulen-7-amine Analogues and the Discovery of a Radiofluorinated 2,3,4,5-Tetrahydro-1-3-benzazepine Congener for Imaging GluN2B Subunit-Containing -Methyl-d-aspartate Receptors.2,3,4,5-四氢-1-3-苯并氮杂䓬和 6,7,8,9-四氢-5-苯并[7]氮杂双环[7.1.0]壬-7-胺类似物的结构亲和力关系及用于成像含 GluN2B 亚基的 -甲基-d-天冬氨酸受体的放射性氟化 2,3,4,5-四氢-1-3-苯并氮杂䓬同系物的发现。
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三种新型 GluN2B 包含型 NMDA 受体放射性示踪剂在非人灵长类动物中的比较：-[C]NR2B-Me、-[F]of-Me-NB1 和 -[F]of-NB1。

Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: -[C]NR2B-Me, -[F]of-Me-NB1, and -[F]of-NB1.

机构信息

Yale School of Medicine, Yale PET Center, New Haven, Connecticut, USA.

Department of Radiology and Biomedical Imaging, Yale School of Medicine, New Haven, USA.

出版信息

J Cereb Blood Flow Metab. 2022 Aug;42(8):1398-1409. doi: 10.1177/0271678X221084416. Epub 2022 Feb 25.

DOI:10.1177/0271678X221084416
PMID:35209743
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9274863/
Abstract

The NMDA receptor GluN2B subunit is a target of interest in neuropsychiatric disorders but to date there is no selective radiotracer available to quantify its availability . Here we report direct comparisons in non-human primates of three GluN2B-targeting radioligands: -[C]NR2B-Me, -[F]OF-Me-NB1, and -[F]OF-NB1. Plasma free fraction, metabolism, tissue distribution and kinetics, and quantitative kinetic modeling methods and parameters were evaluated in two adult rhesus macaques. Free fraction in plasma was <2% for -[C]NR2B-Me and -[F]OF-Me-NB1 and higher for -[F]OF-NB1 (15%). All radiotracers showed good brain uptake and distribution throughout grey matter, with substantial (>68%) blockade across the brain by the GluN2B-targeting drug Co-101,244 (0.25 mg/kg), including in the cerebellum. Time-activity curves were well-fitted by the one-tissue compartment model, with volume of distribution values of 20-40 mL/cm for -[C]NR2B-Me, 8-16 mL/cm for -[F]OF-Me-NB1, and 15-35 mL/cm for -[F]OF-NB1. Estimates of regional non-displaceable binding potential were in the range of 2-3 for -[C]NR2B-Me and -[F]-OF-NB1, and 0.5-1 for -[F]OF-Me-NB1. Altogether, each radiotracer showed an acceptable profile for quantitative imaging of GluN2B. -[F]OF-NB1 has particularly promising imaging characteristics for potential translation into humans. However, the source of unexpected displaceable binding in the cerebellum for each of these compounds requires further investigation.

摘要

NMDA 受体 GluN2B 亚基是神经精神疾病的研究靶点，但目前尚无可用的选择性放射性示踪剂来定量其可用性。在此，我们在非人类灵长类动物中直接比较了三种 GluN2B 靶向放射性配体：-[C]NR2B-Me、-[F]OF-Me-NB1 和-[F]OF-NB1。在两只成年恒河猴中评估了其血浆游离分数、代谢、组织分布和动力学以及定量动力学建模方法和参数。-[C]NR2B-Me 和-[F]OF-Me-NB1 的血浆游离分数<2%，而-[F]OF-NB1 的血浆游离分数较高（15%）。所有放射性示踪剂在大脑中的摄取和分布均良好，且 GluN2B 靶向药物 Co-101,244（0.25mg/kg）可使大脑中放射性示踪剂的分布阻断>68%，包括小脑。放射性示踪剂的时间-活性曲线均由单室模型拟合，-[C]NR2B-Me 的分布容积值为 20-40mL/cm，-[F]OF-Me-NB1 的为 8-16mL/cm，-[F]OF-NB1 的为 15-35mL/cm。-[C]NR2B-Me 和-[F]OF-NB1 的估计区域非占有率结合量在 2-3 之间，而-[F]OF-Me-NB1 的在 0.5-1 之间。总的来说，每种放射性示踪剂在 GluN2B 的定量成像方面均表现出可接受的特征。-[F]OF-NB1 具有特别有前景的成像特征，可能适合转化为人类研究。然而，这些化合物在小脑中出现意外可置换结合的原因仍需进一步研究。