用于大麻素受体正电子发射断层显像（PET）成像的[F]FMPEP-的自动化放射性合成
Automated radiosynthesis of [F]FMPEP- for cannabinoid receptor PET imaging.
作者信息
Jiang Huailei, Guo Yan, Muzik Otto
机构信息
Cyclotron and Radiochemistry Core, Karmanos Cancer Institute Detroit, MI, USA.
PET Center, Karmanos Cancer Institute Detroit, MI, USA.
出版信息
Am J Nucl Med Mol Imaging. 2023 Aug 15;13(4):171-178. eCollection 2023.
Abstract
The cannabinoid subtype 1 receptor (CB1R) is highly expressed in the central nervous system and abnormalities in regional CB1R density are associated with neurodegenerative disorders. The PET tracer [F]FMPEP- is an inverse CB1R agonist which was shown to be suitable for non-invasive PET imaging. In this work, we reported the fully automated radiosynthesis of [F]FMPEP- on a Synthra RNplus research module. In a total synthesis time of 70 min, [F]FMPEP- was obtained in 2.2 ± 0.1 GBq (n = 3) with excellent radiochemical and chemical purity. Quality control test showed that [F]FMPEP- product meets all the release criteria for clinical patient use.
摘要
大麻素1型受体（CB1R）在中枢神经系统中高度表达，区域CB1R密度异常与神经退行性疾病有关。正电子发射断层扫描（PET）示踪剂[F]FMPEP-是一种CB1R反向激动剂，已证明适用于非侵入性PET成像。在本研究中，我们报道了在Synthra RNplus研究模块上实现[F]FMPEP-的全自动放射性合成。在总合成时间70分钟内，获得了[F]FMPEP-，活度为2.2±0.1 GBq（n = 3），放射化学纯度和化学纯度均优异。质量控制测试表明，[F]FMPEP-产品符合临床患者使用的所有放行标准。
相似文献
1
Automated radiosynthesis of [F]FMPEP- for cannabinoid receptor PET imaging.用于大麻素受体正电子发射断层显像（PET）成像的[F]FMPEP-的自动化放射性合成
Am J Nucl Med Mol Imaging. 2023 Aug 15;13(4):171-178. eCollection 2023.
2
Automated GMP production and long-term experience in radiosynthesis of CB tracer [ F]FMPEP-d.自动化 GMP 生产及 [ F]FMPEP-d 放射性示踪剂合成的长期经验。
J Labelled Comp Radiopharm. 2020 Jul;63(9):408-418. doi: 10.1002/jlcr.3845. Epub 2020 Jul 1.
3
[F]FMPEP-d PET imaging shows age- and genotype-dependent impairments in the availability of cannabinoid receptor 1 in a mouse model of Alzheimer's disease.[F]FMPEP-d PET 成像显示，在阿尔茨海默病小鼠模型中，大麻素受体 1 的可用性存在年龄和基因型依赖性损伤。
Neurobiol Aging. 2018 Sep;69:199-208. doi: 10.1016/j.neurobiolaging.2018.05.013. Epub 2018 May 18.
4
Automated radiosynthesis of [ F]CETO, a PET radiotracer for imaging adrenal glands, on Synthra RNplus.在Synthra RNplus上自动放射性合成用于肾上腺成像的正电子发射断层显像（PET）放射性示踪剂[F]CETO。
J Labelled Comp Radiopharm. 2024 Feb;67(2):67-75. doi: 10.1002/jlcr.4078. Epub 2023 Dec 20.
5
[18F]FMeNER-D2: reliable fully-automated synthesis for visualization of the norepinephrine transporter.[18F]FMeNER-D2：用于可视化去甲肾上腺素转运体的可靠全自动合成。
Nucl Med Biol. 2013 Nov;40(8):1049-54. doi: 10.1016/j.nucmedbio.2013.08.007. Epub 2013 Oct 5.
6
Fully automated radiosynthesis and quality control of estrogen receptor targeting radiopharmaceutical 16α-[F]fluoroestradiol ([F]FES) for human breast cancer imaging.全自动合成及质量控制用于人类乳腺癌成像的雌激素受体靶向放射性药物 16α-[F]氟雌二醇([F]FES)
Appl Radiat Isot. 2020 Jun;160:109109. doi: 10.1016/j.apradiso.2020.109109. Epub 2020 Mar 3.
7
Automated production of [F]Flortaucipir for PET imaging of tauopathies.用于tau蛋白病PET成像的[F]氟代托卡朋的自动化生产。
Am J Nucl Med Mol Imaging. 2021 Jun 15;11(3):167-177. eCollection 2021.
8
Automated radiosynthesis of 1-(2-[ F]fluoroethyl)-L-tryptophan ([ F]FETrp) for positron emission tomography (PET) imaging of cancer in humans.自动化合成用于正电子发射断层扫描（PET）成像人类癌症的 1-(2-[F]氟乙基)-L-色氨酸 ([F]FETrp)。
J Labelled Comp Radiopharm. 2023 Jun;66(7-8):180-188. doi: 10.1002/jlcr.4027. Epub 2023 May 11.
9
Cannabinoid Receptor Type 1 in Parkinson's Disease: A Positron Emission Tomography Study with [ F]FMPEP-d.大麻素受体 1 在帕金森病中的作用：[ F]FMPEP-d 的正电子发射断层扫描研究。
Mov Disord. 2022 Aug;37(8):1673-1682. doi: 10.1002/mds.29117. Epub 2022 Jun 8.
10
Automated radiosynthesis of [C]CPPC for in-human PET imaging applications.用于人体正电子发射断层显像（PET）成像应用的[C]CPPC的自动化放射性合成。
Am J Nucl Med Mol Imaging. 2024 Apr 25;14(2):144-148. doi: 10.62347/MXKZ6739. eCollection 2024.
引用本文的文献
1
Noninvasive PET imaging of tumor PD-L1 expression with Cu-labeled Durvalumab.用铜标记的度伐鲁单抗对肿瘤程序性死亡受体配体1（PD-L1）表达进行无创正电子发射断层扫描（PET）成像
Am J Nucl Med Mol Imaging. 2024 Feb 20;14(1):31-40. doi: 10.62347/HUQD8000. eCollection 2024.
本文引用的文献
1
Automated radiosynthesis of 1-(2-[ F]fluoroethyl)-L-tryptophan ([ F]FETrp) for positron emission tomography (PET) imaging of cancer in humans.自动化合成用于正电子发射断层扫描（PET）成像人类癌症的 1-(2-[F]氟乙基)-L-色氨酸 ([F]FETrp)。
J Labelled Comp Radiopharm. 2023 Jun;66(7-8):180-188. doi: 10.1002/jlcr.4027. Epub 2023 May 11.
2
Radiosynthesis and validation of [ F]fluoroestradiol in a Synthra plus research platform for use in routine clinical practice.在 Synthra plus 研究平台上进行 [ F]氟雌二醇的放射性合成和验证，以用于常规临床实践。
J Labelled Comp Radiopharm. 2022 Aug;65(10-11):292-297. doi: 10.1002/jlcr.3998. Epub 2022 Sep 5.
3
Automated production of [F]Flortaucipir for PET imaging of tauopathies.用于tau蛋白病PET成像的[F]氟代托卡朋的自动化生产。
Am J Nucl Med Mol Imaging. 2021 Jun 15;11(3):167-177. eCollection 2021.
4
Automated GMP production and long-term experience in radiosynthesis of CB tracer [ F]FMPEP-d.自动化 GMP 生产及 [ F]FMPEP-d 放射性示踪剂合成的长期经验。
J Labelled Comp Radiopharm. 2020 Jul;63(9):408-418. doi: 10.1002/jlcr.3845. Epub 2020 Jul 1.
5
Cannabinoids and the expanded endocannabinoid system in neurological disorders.大麻素与神经系统疾病中的扩展内源性大麻素系统。
Nat Rev Neurol. 2020 Jan;16(1):9-29. doi: 10.1038/s41582-019-0284-z. Epub 2019 Dec 12.
6
In Vivo Availability of Cannabinoid 1 Receptor Levels in Patients With First-Episode Psychosis.首发精神病患者大麻素 1 受体水平的体内可用性。
JAMA Psychiatry. 2019 Oct 1;76(10):1074-1084. doi: 10.1001/jamapsychiatry.2019.1427.
7
Cannabinoid Type 1 Receptors Are Upregulated During Acute Activation of Brown Adipose Tissue.大麻素受体 1 在棕色脂肪组织急性激活期间上调。
Diabetes. 2018 Jul;67(7):1226-1236. doi: 10.2337/db17-1366. Epub 2018 Apr 12.
8
Endocannabinoid System: the Direct and Indirect Involvement in the Memory and Learning Processes-a Short Review.内源性大麻素系统：在记忆和学习过程中的直接和间接参与——简要综述。
Mol Neurobiol. 2017 Dec;54(10):8332-8347. doi: 10.1007/s12035-016-0313-5. Epub 2016 Dec 6.
9
The endocannabinoid system in guarding against fear, anxiety and stress.内源性大麻素系统在预防恐惧、焦虑和压力方面的作用。
Nat Rev Neurosci. 2015 Dec;16(12):705-18. doi: 10.1038/nrn4036.
10
Cognitive reserve and clinical expression of Alzheimer's disease: evidence and implications for brain PET imaging.认知储备与阿尔茨海默病的临床表型：脑PET成像的证据及意义
Am J Nucl Med Mol Imaging. 2014 Apr 25;4(3):239-47. eCollection 2014.
Zotero 插件