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Literature DB >> 25279444

Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors.

Xiaoyun Zhou¹, Shivashankar Khanapur, Anja P Huizing, Rolf Zijlma, Marianne Schepers, Rudi A J O Dierckx, Aren van Waarde, Erik F J de Vries, Philip H Elsinga.

Abstract

2-(2-Furanyl)-7-[2-[4-[4-(2-[(11)C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine [(11)C]-3 ([(11)C]Preladenant) was developed for mapping cerebral adenosine A2A receptors (A2ARs) with PET. The tracer was synthesized in high specific activity and purity. Tissue distribution was studied by PET imaging, ex vivo biodistribution (BD), and in vitro autoradiography (ARG) experiments. Regional brain uptake of [(11)C]-3 was consistent with known A2ARs distribution, with highest uptake in striatum. The results indicate that [(11)C]-3 has favorable brain kinetics and exhibits suitable characteristics as an A2AR PET tracer.

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Year: 2014 PMID： 25279444 DOI： 10.1021/jm501065t

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

8 in total

1. In vivo evaluation of [¹¹C]preladenant positron emission tomography for quantification of adenosine A_2A receptors in the rat brain.

Authors: Xiaoyun Zhou; Shivashankar Khanapur; Johan R de Jong; Antoon Tm Willemsen; Rudi Ajo Dierckx; Philip H Elsinga; Erik Fj de Vries
Journal: J Cereb Blood Flow Metab Date: 2016-07-20 Impact factor: 6.200

2. Radiation Dosimetry of a Novel Adenosine A_2A Receptor Radioligand [¹¹C]Preladenant Based on PET/CT Imaging and Ex Vivo Biodistribution in Rats.

Authors: Xiaoyun Zhou; Philip H Elsinga; Shivashankar Khanapur; Rudi A J O Dierckx; Erik F J de Vries; Johan R de Jong
Journal: Mol Imaging Biol Date: 2017-04 Impact factor: 3.488

3. Bitopic fluorescent antagonists of the A_2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.

Authors: Romain Duroux; Antonella Ciancetta; Philip Mannes; Jinha Yu; Shireesha Boyapati; Elizabeth Gizewski; Said Yous; Francisco Ciruela; John A Auchampach; Zhan-Guo Gao; Kenneth A Jacobson
Journal: Medchemcomm Date: 2017-06-22 Impact factor: 3.597

Review 8. Allosteric Interactions between Adenosine A_2A and Dopamine D₂ Receptors in Heteromeric Complexes: Biochemical and Pharmacological Characteristics, and Opportunities for PET Imaging.

Authors: Kavya Prasad; Erik F J de Vries; Philip H Elsinga; Rudi A J O Dierckx; Aren van Waarde
Journal: Int J Mol Sci Date: 2021-02-09 Impact factor: 5.923

8 in total

Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors.

1. In vivo evaluation of [¹¹C]preladenant positron emission tomography for quantification of adenosine A_2A receptors in the rat brain.

2. Radiation Dosimetry of a Novel Adenosine A_2A Receptor Radioligand [¹¹C]Preladenant Based on PET/CT Imaging and Ex Vivo Biodistribution in Rats.

3. Bitopic fluorescent antagonists of the A_2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.

Review 4. Chemical Probes for the Adenosine Receptors.

Review 5. Tracers for non-invasive radionuclide imaging of immune checkpoint expression in cancer.

Review 6. Molecular probes for the human adenosine receptors.

Review 7. In Vivo Positron Emission Tomography Imaging of Adenosine A_2A Receptors.

Review 8. Allosteric Interactions between Adenosine A_2A and Dopamine D₂ Receptors in Heteromeric Complexes: Biochemical and Pharmacological Characteristics, and Opportunities for PET Imaging.

Synthesis and preclinical evaluation of 2-(2-furanyl)-7-[2-[4-[4-(2-[11C]methoxyethoxy)phenyl]-1-piperazinyl]ethyl]7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine-5-amine ([11C]Preladenant) as a PET tracer for the imaging of cerebral adenosine A2A receptors.

1. In vivo evaluation of [11C]preladenant positron emission tomography for quantification of adenosine A2A receptors in the rat brain.

2. Radiation Dosimetry of a Novel Adenosine A2A Receptor Radioligand [11C]Preladenant Based on PET/CT Imaging and Ex Vivo Biodistribution in Rats.

3. Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.

Review 4. Chemical Probes for the Adenosine Receptors.

Review 5. Tracers for non-invasive radionuclide imaging of immune checkpoint expression in cancer.

Review 6. Molecular probes for the human adenosine receptors.

Review 7. In Vivo Positron Emission Tomography Imaging of Adenosine A2A Receptors.

Review 8. Allosteric Interactions between Adenosine A2A and Dopamine D2 Receptors in Heteromeric Complexes: Biochemical and Pharmacological Characteristics, and Opportunities for PET Imaging.

1. In vivo evaluation of [¹¹C]preladenant positron emission tomography for quantification of adenosine A_2A receptors in the rat brain.

2. Radiation Dosimetry of a Novel Adenosine A_2A Receptor Radioligand [¹¹C]Preladenant Based on PET/CT Imaging and Ex Vivo Biodistribution in Rats.

3. Bitopic fluorescent antagonists of the A_2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.

Review 7. In Vivo Positron Emission Tomography Imaging of Adenosine A_2A Receptors.

Review 8. Allosteric Interactions between Adenosine A_2A and Dopamine D₂ Receptors in Heteromeric Complexes: Biochemical and Pharmacological Characteristics, and Opportunities for PET Imaging.