Literature DB >> 24291040

Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.

Laurent Hortala1, Joëlle Arnaud1, Pascale Roux1, Didier Oustric1, Laurent Boulu1, Florence Oury-Donat1, Patrick Avenet2, Thomas Rooney3, David Alagille4, Olivier Barret4, Gilles Tamagnan4, Francis Barth5.   

Abstract

Cannabinoid CB2 PET tracers are considered as a promising alternative to PBR/TSPO tracers for the in-vivo imaging of neuroinflammation. We describe here the synthesis and characterization of compound 3, a new potent and brain penetrating CB2 ligand based on an original triazine template. The PET tracer [(18)F]-dideutero-3 was prepared in a three steps radiosynthesis, and demonstrated significant uptake in rhesus macaque and baboon brain with a maximum SUV of about 0.7-0.9g/mL, followed by a moderate washout over time.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  CB2; Cannabinoid; Imaging; PET; Triazine

Mesh:

Substances:

Year:  2013        PMID: 24291040     DOI: 10.1016/j.bmcl.2013.11.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

1.  Decreased in vivo availability of the cannabinoid type 2 receptor in Alzheimer's disease.

Authors:  Rawaha Ahmad; Andrey Postnov; Guy Bormans; Jan Versijpt; Mathieu Vandenbulcke; Koen Van Laere
Journal:  Eur J Nucl Med Mol Imaging       Date:  2016-08-03       Impact factor: 9.236

2.  PET Imaging of the P2X7 Ion Channel with a Novel Tracer [18F]JNJ-64413739 in a Rat Model of Neuroinflammation.

Authors:  Tamara Berdyyeva; Chunfang Xia; Natalie Taylor; Yingbo He; Gang Chen; Chaofeng Huang; Wei Zhang; Hartmuth Kolb; Michael Letavic; Anindya Bhattacharya; Anna Katrin Szardenings
Journal:  Mol Imaging Biol       Date:  2019-10       Impact factor: 3.488

Review 3.  Role of neuro-immunological factors in the pathophysiology of mood disorders.

Authors:  Anindya Bhattacharya; Noel C Derecki; Timothy W Lovenberg; Wayne C Drevets
Journal:  Psychopharmacology (Berl)       Date:  2016-01-23       Impact factor: 4.530

4.  Expression of functional cannabinoid CB2 receptor in VTA dopamine neurons in rats.

Authors:  Hai-Ying Zhang; Ming Gao; Hui Shen; Guo-Hua Bi; Hong-Ju Yang; Qing-Rong Liu; Jie Wu; Eliot L Gardner; Antonello Bonci; Zheng-Xiong Xi
Journal:  Addict Biol       Date:  2016-02-01       Impact factor: 4.280

Review 5.  Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development.

Authors:  Lu Hou; Jian Rong; Ahmed Haider; Daisuke Ogasawara; Cassis Varlow; Michael A Schafroth; Linjing Mu; Jiefeng Gan; Hao Xu; Christopher J Fowler; Ming-Rong Zhang; Neil Vasdev; Simon Ametamey; Benjamin F Cravatt; Lu Wang; Steven H Liang
Journal:  J Med Chem       Date:  2020-12-30       Impact factor: 7.446

6.  Cannabinoid CB2 Receptors in a Mouse Model of Aβ Amyloidosis: Immunohistochemical Analysis and Suitability as a PET Biomarker of Neuroinflammation.

Authors:  Alena V Savonenko; Tatiana Melnikova; Yuchuan Wang; Hayden Ravert; Yongjun Gao; Jeremy Koppel; Deidre Lee; Olga Pletnikova; Eugenia Cho; Nuzhat Sayyida; Andrew Hiatt; Juan Troncoso; Peter Davies; Robert F Dannals; Martin G Pomper; Andrew G Horti
Journal:  PLoS One       Date:  2015-06-18       Impact factor: 3.240

Review 7.  Molecular Targets for PET Imaging of Activated Microglia: The Current Situation and Future Expectations.

Authors:  Claire Tronel; Bérenger Largeau; Maria Joao Santiago Ribeiro; Denis Guilloteau; Anne-Claire Dupont; Nicolas Arlicot
Journal:  Int J Mol Sci       Date:  2017-04-11       Impact factor: 5.923

8.  Synthesis and Biological Evaluation of Thiophene-Based Cannabinoid Receptor Type 2 Radiotracers for PET Imaging.

Authors:  Ahmed Haider; Adrienne Müller Herde; Roger Slavik; Markus Weber; Claudia Mugnaini; Alessia Ligresti; Roger Schibli; Linjing Mu; Simon Mensah Ametamey
Journal:  Front Neurosci       Date:  2016-07-27       Impact factor: 4.677

Review 9.  Targeting Cannabinoid CB2 Receptors in the Central Nervous System. Medicinal Chemistry Approaches with Focus on Neurodegenerative Disorders.

Authors:  Gemma Navarro; Paula Morales; Carmen Rodríguez-Cueto; Javier Fernández-Ruiz; Nadine Jagerovic; Rafael Franco
Journal:  Front Neurosci       Date:  2016-09-13       Impact factor: 4.677

  9 in total

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