Jakobsson Jimmy E, Gourni Eleni, Khanapur Shivashankar, Brito Beatriz, Riss Patrick J
Realomics SRI, Kjemisk Institutt, Universitetet i Oslo, Sem Sælands vei 26, Kjemibygningen, 0371 Oslo, Norway.
Norsk Medisinsk Syklotronsenter AS, Gaustad, Postboks 4950 Nydalen, 0424 Oslo, Norway.
ACS Omega. 2019 Jun 6;4(6):9925-9931. doi: 10.1021/acsomega.9b00357. eCollection 2019 Jun 30.
The NR2B subunit of the -methyl-d-aspartate (NMDA) receptor has been implicated in controlling synaptic plasticity, memory, and learning. Herein, we describe an C-labeled PET radiotracer based on 1-(4-chlorophenethyl)-6-methoxy-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-ol, Ro04-5595. The radiotracer was evaluated in rats using PET. The PET study showed a good pharmacokinetic profile with rapid uptake and washout over 90 min. Complementary high-resolution autoradiographic images using [H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low. We conclude to have developed a selective NR2B receptor radioligand suitable for quantitative and qualitative imaging of a NR2B receptor distribution in vitro and in vivo.
N-甲基-D-天冬氨酸（NMDA）受体的NR2B亚基与控制突触可塑性、记忆和学习有关。在此，我们描述了一种基于1-(4-氯苯乙基)-6-甲氧基-2-甲基-1,2,3,4-四氢异喹啉-7-醇（Ro04-5595）的碳-11标记的正电子发射断层扫描（PET）放射性示踪剂。该放射性示踪剂在大鼠中使用PET进行了评估。PET研究显示出良好的药代动力学特征，在90分钟内摄取和清除迅速。使用[氢]Ro04-5595的补充高分辨率放射自显影图像显示，在富含NR2B受体的区域有强烈结合，而在NR2B浓度较低的小脑中结合较弱。我们得出结论，已开发出一种选择性NR2B受体放射性配体，适用于体外和体内NR2B受体分布的定量和定性成像。
