Výsledky vyhledávání - "Gilles, Tamagnan"

Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: (R)-[11C]NR2B-Me, (R)-[18F]of-Me-NB1, and (S)-[18F]of-NB1

Autor: Kelly Smart, Ming-Qiang Zheng, Hazem Ahmed, Hanyi Fang, Yuping Xu, Lisheng Cai, Daniel Holden, Michael Kapinos, Ahmed Haider, Zachary Felchner, Jim R Ropchan, Gilles Tamagnan, Robert B Innis, Victor W Pike, Simon M Ametamey, Yiyun Huang, Richard E Carson

Publikováno v: J Cereb Blood Flow Metab

The NMDA receptor GluN2B subunit is a target of interest in neuropsychiatric disorders but to date there is no selective radiotracer available to quantify its availability in vivo. Here we report direct comparisons in non-human primates of three GluN

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::623b232517415f95404387a58ac3b9bc
https://doi.org/10.1177/0271678x221084416

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Preclinical characterization of [18F]T-008, a novel PET imaging radioligand for cholesterol 24-hydroxylase

Autor: Cristian Constantinescu, David Alagille, Caroline Papin, Eiji Sunahara, Shuhei Ikeda, Tatsuki Koike, Maki Miyamoto, John Seibyl, Gilles Tamagnan, Olivier Barret, Thomas J. Morley, Krista Fowles, Patricia E. Cole, Takanobu Kuroita, Toshiya Nishi

Publikováno v: European Journal of Nuclear Medicine and Molecular Imaging. 49:1148-1156

Purpose Cholesterol 24-hydroxylase (CH24H) is a brain-specific enzyme that plays a major role in brain cholesterol homeostasis by converting cholesterol into 24S-hydroxycholesterol. The selective CH24H inhibitor soticlestat (TAK-935) is being pursued

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8c3b49ad503abe1c9b276111d06b8346
https://doi.org/10.1007/s00259-021-05565-z

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Design, Synthesis, and Evaluation of [18F]T-914 as a Novel Positron-Emission Tomography Tracer for Lysine-Specific Demethylase 1

Autor: Tohru Yamashita, Tatsuki Koike, Haruhide Kimura, Gilles Tamagnan, Kouta Matsumiya, Jumpei Aida, Olivier Barret, Yasushi Hattori, Paul McQuade, Satoru Matsuda, Christine M Sandiego, Alexandra Gouasmat, Vincent M. Carroll

Publikováno v: Journal of Medicinal Chemistry. 64:12680-12690

Histone methylation is associated with the pathophysiology of neurodevelopmental disorders. Lysine-specific demethylase 1 (LSD1) catalyzes histone demethylation in a flavin adenine dinucleotide (FAD)-dependent manner. Thus, inhibiting LSD1 enzyme act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e9d128461b397c8eb721e36a82043d7b
https://doi.org/10.1021/acs.jmedchem.1c00653

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Design, Synthesis, and Evaluation of (2-Aminocyclopropyl)phenyl Derivatives as Novel Positron Emission Tomography Imaging Agents for Lysine-Specific Demethylase 1 in the Brain

Autor: David Alagille, Satoru Matsuda, Rina Baba, Gilles Tamagnan, Thomas J. Morley, Yasushi Hattori, Tatsuki Koike, Caroline Papin, Cristian Constantinescu, Alexandra Gouasmat, Vincent M. Carroll, Shinji Iwasaki, Kouta Matsumiya

Publikováno v: Journal of Medicinal Chemistry. 64:3780-3793

Dysregulation of histone H3 lysine 4 (H3K4) methylation is implicated in the pathogenesis of neurodevelopmental disorders. Lysine-specific demethylase 1 (LSD1) determines the methylation status of H3K4 through flavin adenine dinucleotide (FAD)-mediat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db440a3e94e4141daeec35dfc6807678
https://doi.org/10.1021/acs.jmedchem.0c01937

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Dopamine D1 Receptor Agonist PET Tracer Development: Assessment in Nonhuman Primates

Autor: Vincent M. Carroll, David Gray, John Seibyl, Olivier Barret, Gilles Tamagnan, Timothy J. McCarthy, Lei Zhang, Jenna M. Sullivan, David Alagille, Caroline Papin, Christine M. Sandiego, Cristian Constantinescu, Jianqing Chen, Anabella Villalobos, Thomas J. Morley, Chewah Lee

Publikováno v: Journal of Nuclear Medicine. 62:1307-1313

Non–catechol-based high-affinity selective dopamine D1 receptor (D1R) agonists were recently described, and candidate PET ligands were selected on the basis of favorable properties. The objective of this study was to characterize in vivo in nonhuma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ab34abe7cd7c382705fc60cac95e5e16
https://doi.org/10.2967/jnumed.120.256008

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Evaluation of (

Autor: Hazem, Ahmed, Ming-Qiang, Zheng, Kelly, Smart, Hanyi, Fang, Li, Zhang, Paul R, Emery, Hong, Gao, Jim, Ropchan, Ahmed, Haider, Gilles, Tamagnan, Richard E, Carson, Simon M, Ametamey, Yiyun, Huang

Publikováno v: J Nucl Med

Despite 2 decades of research, no N-methyl-d-aspartate (NMDA) glutamate receptor (GluN) subtype 2B (GluN1/2B) radioligand is yet clinically validated. Previously, we reported on (rac)-(18)F-OF-NB1 as a promising GluN1/2B PET probe in rodents and its

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::728ce1ecd0ae4dc51f54206a535f2882
https://pubmed.ncbi.nlm.nih.gov/35710735

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Characterization in Non-human Primates of (R)-[18F]OF-Me-NB1 and (S)-[18F]OF-Me-NB1 for Imaging the GluN2B Subunits of the NMDA Receptor

Autor: Yiyun Huang, Zachary Felchner, Ming-Qiang Zheng, Daniel Holden, Michael Kapinos, Richard Carson, Hazem Ahmed, Kelly Smart, Gilles Tamagnan, Simon M. Ametamey, Yuping Xu, Ahmed Haider

Purpose GluN2B containing N-methyl-D-aspartate receptors (NMDARs) play an essential role in neurotransmission and are a potential treatment target for multiple neurological and neurodegenerative diseases, including stroke, Alzheimer’s disease, and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b705781a7cd0de6fbec4dfb640f3c100
https://doi.org/10.21203/rs.3.rs-1068936/v1

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Characterization in nonhuman primates of (R)-[

Autor: MingQiang, Zheng, Hazem, Ahmed, Kelly, Smart, Yuping, Xu, Daniel, Holden, Michael, Kapinos, Zachary, Felchner, Ahmed, Haider, Gilles, Tamagnan, Richard E, Carson, Yiyun, Huang, Simon M, Ametamey

Publikováno v: European journal of nuclear medicine and molecular imaging. 49(7)

GluN2B containing N-methyl-D-aspartate receptors (NMDARs) play an essential role in neurotransmission and are a potential treatment target for multiple neurological and neurodegenerative diseases, including stroke, Alzheimer's disease, and Parkinson'

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::64f097e70e45fe3cfa9958ab31fe7d6a
https://pubmed.ncbi.nlm.nih.gov/35107627

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Design and synthesis of aryl-piperidine derivatives as potent and selective PET tracers for cholesterol 24-hydroxylase (CH24H)

Autor: Shuhei Ikeda, Yuichi Kajita, Maki Miyamoto, Kouta Matsumiya, Tsuyoshi Ishii, Toshiya Nishi, Sean C. Gay, Weston Lane, Cristian C. Constantinescu, David Alagille, Caroline Papin, Gilles Tamagnan, Takanobu Kuroita, Tatsuki Koike

Publikováno v: European Journal of Medicinal Chemistry. 240:114612

Cholesterol 24-hydroxylase (CH24H, CYP46A1) is a cytochrome P450 family enzyme that maintains the homeostasis of brain cholesterol. Soticlestat, a potent and selective CH24H inhibitor, is in development as a therapeutic agent for Dravet syndrome and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9071b5554959d9fd9754f52119b076b2
https://doi.org/10.1016/j.ejmech.2022.114612

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