Binding characterization of N‐(2‐chloro‐5‐thiomethylphenyl)‐N′‐(3‐[3H]3methoxy phenyl)‐N′‐methylguanidine ([3H]GMOM), a non‐competitive N‐methyl‐D‐aspartate (NMDA) receptor antagonist

Autor: Athanasios Metaxas, Bart N. M. van Berckel, Pieter J. Klein, Joost Verbeek, Emily C. Nash, Esther J. M. Kooijman, Véronique A. Renjaän, Sandeep S. V. Golla, Ronald Boellaard, Johannes A. M. Christiaans, Albert D. Windhorst, Josée E. Leysen

Publikováno v: Pharmacology Research & Perspectives, Vol 7, Iss 1, Pp n/a-n/a (2019)

Abstract Labeled with carbon‐11, N‐(2‐chloro‐5‐thiomethylphenyl)‐N′‐(3‐methoxyphenyl)‐N′‐methylguanidine ([11C]GMOM) is currently the only positron emission tomography (PET) tracer that has shown selectivity for the ion‐chan

Externí odkaz: https://doaj.org/article/d526cd10484549bca728a435a4c3653a

Synthesis, radiolabeling and preclinical evaluation of a [11C]GMOM derivative as PET radiotracer for the ion channel of the N-methyl-D-aspartate receptor

Autor: Johannes A. M. Christiaans, Esther J.M. Kooijman, Bart N.M. van Berckel, Albert D. Windhorst, Pieter J. Klein, Athanasios Metaxas, Adriaan A. Lammertsma, Robert C. Schuit

Publikováno v: Klein, P J, Schuit, R C, Metaxas, A, Christiaans, J AM, Kooijman, E, Lammertsma, A A, van Berckel, B NM & Windhorst, A D 2017, ' Synthesis, radiolabeling and preclinical evaluation of a [ 11 C]GMOM derivative as PET radiotracer for the ion channel of the N-methyl-D-aspartate receptor ', Nuclear Medicine and Biology, vol. 51, pp. 25-32 . https://doi.org/10.1016/j.nucmedbio.2017.05.003
Nuclear Medicine and Biology, 51, 25-32. Elsevier Inc.

Introduction Presently available PET ligands for the NMDAr ion channel generally suffer from fast metabolism. The purpose of this study was to develop a metabolically more stable ligand for the NMDAr ion channel, taking [11C]GMOM ([11C]1) as the lead

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ceb0b4933edff4a728bc8b7ba2314f9b
https://doi.org/10.1016/j.nucmedbio.2017.05.003

Quantification of the novel N-methyl-D-aspartate receptor ligand [C-11] GMOM in man

Autor: Thalia F. van der Doef, Pieter J. Klein, Athanasios Metaxas, Bart N.M. van Berckel, Gisela M. Oropeza-Seguias, Ellen Jobse, Sandeep S.V. Golla, Albert D. Windhorst, Robert C. Schuit, Adriaan A. Lammertsma, Ronald Boellaard, Lothar A. Schwarte

Publikováno v: Journal of Cerebral Blood Flow and Metabolism, 36(6), 1111-1121. Nature Publishing Group
Journal of Cerebral Blood Flow & Metabolism
van der Doef, T F, Golla, S S V, Klein, P J, Oropeza-Seguias, G M, Schuit, R C, Metaxas, A, Jobse, E, Schwarte, L A, Windhorst, A D, Lammertsma, A A, van Berckel, B N M & Boellaard, R 2016, ' Quantification of the novel N-methyl-D-aspartate receptor ligand [C-11] GMOM in man ', Journal of Cerebral Blood Flow and Metabolism, vol. 36, no. 6, pp. 1111-1121 . https://doi.org/10.1177/0271678X15608391

[11C]GMOM (carbon-11 labeled N-(2-chloro-5-thiomethylphenyl)- N′-(3-[11C]methoxy-phenyl)- N′-methylguanidine) is a PET ligand that binds to the N-methyl-d-aspartate receptor with high specificity and affinity. The purpose of this first in human s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efe26d5aff0098bfdf4b3c5a1c0e7332
https://doi.org/10.1177/0271678x15608391

Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography

Autor: Pieter J. Klein, Albert D. Windhorst, Adriaan A. Lammertsma, Johannes A. M. Christiaans, Robert C. Schuit, Athanasios Metaxas, B.N.M. van Berckel

Publikováno v: Klein, P J, Christiaans, J A M, Metaxas, A, Schuit, R C, Lammertsma, A A, van Berckel, B N M & Windhorst, A D 2015, ' Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography ', Bioorganic and Medicinal Chemistry, vol. 23, no. 5, pp. 1189-1206 . https://doi.org/10.1016/j.bmc.2014.12.029
Bioorganic and Medicinal Chemistry, 23(5), 1189-1206. Elsevier Limited

The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f9631abf4fb185d88dcf2488adee9a0
https://doi.org/10.1016/j.bmc.2014.12.029

Subchronic treatment with phencyclidine in adolescence leads to impaired exploratory behavior in adult rats without altering social interaction orN-methyl-D-aspartate receptor binding levels

Autor: Pieter J. Klein, Athanasios Metaxas, Josée E. Leysen, Roland Willems, B.N.M. van Berckel, V.A. Renjaän, Albert D. Windhorst, Esther J.M. Kooijman, L. Ver Donck

Publikováno v: Journal of Neuroscience Research. 92:1599-1607

Although both the onset of schizophrenia and human phencyclidine (PCP) abuse typically present within the interval from adolescence to early adulthood, the majority of preclinical research employing the PCP model of schizophrenia has been conducted o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::65f3eb2d7d171bed84b3aeef8152639f
https://doi.org/10.1002/jnr.23433