Synthesis and in vitro evaluation of new translocator protein ligands designed for positron emission tomography-Reference-Cited by-同舟云学术

Synthesis and in vitro evaluation of new translocator protein ligands designed for positron emission tomography

Published:2019-03 Issue:6 Volume:11 Page:539-550
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Kalina Thomas¹,Berroterán-Infante Neydher²³,Schmitl Stefan²,Vraka Chrysoula²,Hacker Marcus²,Mitterhauser Markus²⁴⁵,Pallitsch Katharina¹,Wadsak Wolfgang²³⁶

Affiliation:

1. Department of Organic Chemistry, Faculty of Chemistry, University of Vienna, Vienna, Austria

2. Division of Nuclear Medicine, Department of Biomedical Imaging & Image-guided Therapy, Medical University of Vienna, Vienna, Austria

3. Department of Inorganic Chemistry, Faculty of Chemistry, University of Vienna, Vienna, Austria

4. Department of Pharmaceutical Technology, Faculty of Life Sciences, University of Vienna, Vienna Austria

5. Ludwig Boltzmann Institute Applied Diagnostics, Vienna, Austria

6. Center for Biomarker Research in Medicine, CBmed GmbH, Graz, Austria

Abstract

Aim: Dysregulated levels of the translocator protein TSPO 18 KDa have been reported in several disorders, particularly neurodegenerative diseases. This makes TSPO an interesting target for the development of diagnostic biomarkers. Even though several radioligands have already been developed for in vivo TSPO imaging, the ideal TSPO radiotracer has still not been found. Results: Here, we report the chemical synthesis of a set of new TSPO ligands designed for future application in positron emission tomography, together with the determination of their biological activity and applied 11C-labeling strategy. Conclusion: The lead compound of our series, (R)-[11C]Me@NEBIQUINIDE, showed very promising results and is therefore proposed to be further evaluated under in vivo settings.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

https://www.future-science.com/doi/pdf/10.4155/fmc-2018-0444

Reference56 articles.

1. Translocator protein (18kDa): new nomenclature for the peripheral-type benzodiazepine receptor based on its structure and molecular function

2. Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding.

3. The 18 kDa Translocator Protein, Microglia and Neuroinflammation

4. The peripheral-type benzodiazepine receptor and the cardiovascular system. Implications for drug development

5. Involvement of Peripheral Benzodiazepine Receptor in the Oxidative Stress, Death-Signaling Pathways, and Renal Injury Induced by Ischemia-Reperfusion

Cited by 4 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Structure-based drug design for TSPO: Challenges and opportunities;Biochimie;2024-09

2. Preclinical Evaluation of Novel PET Probes for Dementia;Seminars in Nuclear Medicine;2023-09

3. Insight into the Structural Features of TSPO: Implications for Drug Development;Trends in Pharmacological Sciences;2020-02

4. (R)-[18F]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging;European Journal of Medicinal Chemistry;2019-08