Kontakt

Dr. Rares-Petru Moldovan

Wissen­schaftlicher Mitarbei­ter / Medizinische Chemie / Radiochemie
Experimentelle Neuroonkologische Radiopharmazie
r.moldovanAthzdr.de
Tel.: +49 351 260 4634

Dr. Daniel Gündel

Wissen­schaftlicher Mitarbeiter
Präklinische PET Radiotracer Evaluie­rung
Experimentelle Neuroonkologische Radiopharmazie
d.guendelAthzdr.de
Tel.: +49 351 260 4615

Dr. Winnie Deuther-Conrad

Wissen­schaftliche Mitarbeiterin
Experimentelle Neuroonkologische Radiopharmazie
w.deuther-conradAthzdr.de
Tel.: +49 351 260 4613

PET Imaging of the Human Cannabinoid Receptors Type 2 (CB2R) in the Brain


Cannabinoid receptors are involved in a wide range of physiological mechanisms. There is evidence that cannabinoid type 2 receptors (CB2R) play a central role in neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as in cancer. Therefore, a therapeutic role for cannabinoid receptor ligands in brain diseases and tumour treatment has been suggested. Neuroimaging with positron emission tomography (PET) will provide a better understanding of the involvement of the cannabinoid system in these diseases in living humans. In addition, neuroimaging with 18F-labelled CB receptor ligands will be useful for monitoring treatment effects. CB2R selective radioligands are being developed and evaluated for PET imaging.

Partners

  • Andrew Horti, Johns Hopkins University, Baltimore, USA
  • Guy Bormanns, KU Leuven, Belgium
  • Osama Sabri, Universität Leipzig, Germany
  • Carmen Abate and Marialessandra Contino, Università degli Studi di Bari 'ALDO MORO', Italy
  • Andrej Kovac, Slovak Academy of Sciences, Slovakia
  • Yvonne Bouter and Caroline Bouter, University Medicine Göttingen, Germany
  • Robert Innis and Victor Pike, NIH, USA

Financial Support by

  • Deutsche Forschungsgemeinschaft - DFG
     

Latest Publications

  • Gündel D., Maqbool M., Teodoro R., Ludwig F.-A., Heerklotz A., Toussaint M.,  Deuther-Conrad W., Bormans G., Brust P., Kopka K., Moldovan R.-P. "Development and evaluation of deuterated [18F]JHU94620 isotopologues for the non-invasive assessment of the cannabinoid type 2 receptor in brain" EJNMMI Radiopharmacy and Chemistry 2024, 9:91. https://doi.org/10.1186/s41181-024-00319-2 
Foto: TOC-JHU ©Copyright: Dr. Rares-Petru Moldovan
  • Teodoro R., Gündel D., Deuther-Conrad W., Kazimir A., Toussaint M., Wenzel B., Bormans G., Hey-Hawkins E., Kopka K., Brust P, Moldovan R.-P. "Synthesis, structure activity relationships, radiofluorination and biological evaluation of [18F]RM365, a novel radioligand for imaging the human cannabinoid receptor type 2 (CB2R) in the Brain with PET" J. Med. Chem. 2023, 66, 20, 13991–14010. https://doi.org/10.1021/acs.jmedchem.3c01035 

Foto: TOC ©Copyright: Dr. Rares-Petru Moldovan

  • Ueberham L., Gündel D., Kellert M., Deuther-Conrad W., Ludwig F.- A., Lönnecke P., Kazimir A., Kopka K., Brust P., Moldovan R.-P., Hey-Hawkins E., "Development of the high-affinity carborane-based cannabinoid receptor type 2 PET ligand [18F]LUZ5-d8" J. Med. Chem. 2023, 66, 7, 5242–5260. https://pubs.acs.org/doi/epdf/10.1021/acs.jmedchem.3c00195 

  • Gündel, D.; Deuther-Conrad, W.; Ueberham, L.; Kaur, S.; Otikova, E.; Teodoro, R.; Lai, T. H.; Clauß, O.; Scheunemann, M.; Bormans, G.; Kopka, K.; Bachmann, M.; Brust, P., Moldovan R.-P. "Structure-based design, optimization, and development of [18F]LU13: A novel radioligand for cannabinoid receptor type 2 imaging in the brain with PET" J. Med. Chem. 2022, 65, 13, 9034–9049. https://doi.org/10.1021/acs.jmedchem.2c00256


  • Teodoro, R.; Gündel, D.; Ueberham, L.; Toussaint, M.; Bormans, G.; Brust, P.; Deuther-Conrad, W.; Moldovan, R.-P. "Development of [18F]LU14 for PET imaging of cannabinoid receptor type 2 in the brain" Int. J. Mol. Sci. 22(2021)15, 8051. https://doi.org/10.3390/ijms22158051 



  • Moldovan R.-P, Hausmann K., Deuther-Conrad W., Brust P. "Development of highly affine and selective fluorinated cannabinoid type 2 receptor ligands" ACS Med. Chem. Let. 2017,8, 566–571. https://doi.org/10.1021/acsmedchemlett.7b00129 


  • Moldovan R.-P., Deuther-Conrad W., Horti A., Brust P. "Synthesis and preliminary biological evaluation of indol-3-yl-oxoacetamides as potent cannabinoid receptor type 2 ligands" Molecules, 2017, 22, E77. https://doi.org/10.3390/molecules22010077 


  • Moldovan R.-P., Teodoro R., Gao Y.,  Deuther-Conrad W., Kranz M., Wang Y., Kuwabara H., Nakano M., Valentine H., Fischer S., Pomper M. G., Wong D. F., Dannals R. F., Brust P., Horti A. G. "Development of a High-Affinity PET Radioligand for Imaging Cannabinoid Subtype 2 Receptor" J. Med. Chem. 2016, 59, 17, 7840–7855 https://doi.org/10.1021/acs.jmedchem.6b00554 

Other Publications

  • Moldovan R.-P., Teodoro R., Deuther-Conrad W., Wang Y., Fischer S., Pomper M., Wong D. F., Dannals R. F., Brust P., Horti A. "[18F]JHU94620, a high affinity PET radioligand for imaging of cannabinoid subtype 2 receptors (CB2R)" J. Nucl. Med. 2015, 56, S3, 1048.
  • Donat C. K., Fischer F., Walter B., Deuther-Conrad W.,Bauer R., Brust P. "Early increase of cannabinoid receptor density after experimental traumatic brain injury in the newborn piglet" Acta Neurbiologiae Experimentalis. 2014, 74, 197-210.
  • Teodoro R, Moldovan R.-P., Lueg C, Günther R, Donat CK, Ludwig F-A, Fischer S, Deuther-Conrad W, Wünsch B, Brust P. "Synthesis, 18F-labelling and first biological evaluation of N-aryl-oxadiazolyl-propionamides as potential radioligands for PET imaging of cannabinoid CB2 receptors."  Org. Med. Chem. Lett. 2013, 3:11. https://doi.org/10.1186/2191-2858-3-11 
  • Rühl T., Deuther-Conrad W., Fischer S., Günther R., Hennig L., Krautscheid H., Brust P. "Cannabinoid receptor type 2 (CB2)-selective N-aryl-oxadiazolyl-propionamides: synthesis, radiolabelling, molecular modelling and biological evaluation" Org. Med. Chem. Lett. 2012, 2:32. https://doi.org/10.1186/2191-2858-2-32