Preclinical development of 18F-OF-NB1 for imaging GluN2B-containing N-Methyl-d-Aspartate receptors and its utility as a biomarker for amyotrophic lateral sclerosis
As part of our continuous efforts to develop a suitable 18F-labeled PET radioligand with
improved characteristics for imaging the N-methyl-d-aspartate receptors (NMDARs) subtype …
improved characteristics for imaging the N-methyl-d-aspartate receptors (NMDARs) subtype …
Evaluation of (rac)-,(R)-, and (S)-18F-OF-NB1 for Imaging GluN2B subunit–containing N-Methyl-d-Aspartate receptors in nonhuman primates
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 …
subtype 2B (GluN1/2B) radioligand is yet clinically validated. Previously, we reported on …
Characterization of (R)- and (S)-[18F]OF-NB1 in Rodents as Positron Emission Tomography Probes for Imaging GluN2B Subunit-Containing N-Methyl-d-Aspartate …
H Ahmed, R Wallimann, L Gisler… - ACS Chemical …, 2023 - ACS Publications
The N-methyl-d-aspartate receptor (NMDAR) subtype 2B (GluN1/2B) is implicated in various
neuropathologies. Given the lack of a validated radiofluorinated positron emission …
neuropathologies. Given the lack of a validated radiofluorinated positron emission …
[HTML][HTML] Characterization in nonhuman primates of (R)-[18F]OF-Me-NB1 and (S)-[18F]OF-Me-NB1 for imaging the GluN2B subunits of the NMDA receptor
Abstract Purpose GluN2B containing N-methyl-D-aspartate receptors (NMDARs) play an
essential role in neurotransmission and are a potential treatment target for multiple …
essential role in neurotransmission and are a potential treatment target for multiple …
Identification and preclinical evaluation of a radiofluorinated benzazepine derivative for imaging the GluN2B subunit of the ionotropic NMDA receptor
The previously reported 11C-labeled GluN2B PET radioligand 11C-Me-NB1 served as a
starting point for derivatization and led to the successful development of a radiofluorinated …
starting point for derivatization and led to the successful development of a radiofluorinated …
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 …
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 …
to date there is no selective radiotracer available to quantify its availability in vivo. Here we …
Structure–Affinity Relationships of 2,3,4,5-Tetrahydro-1H-3-benzazepine and 6,7,8,9-Tetrahydro-5H-benzo[7]annulen-7-amine Analogues and the Discovery of a Radiofluorinated 2,3,4,5-Tetrahydro …
Aspiring to develop a positron emission tomography (PET) imaging agent for the GluN2B
subunits of the N-methyl-d-aspartate receptor (NMDAR), a key therapeutic target for drug …
subunits of the N-methyl-d-aspartate receptor (NMDAR), a key therapeutic target for drug …
First-in-humans brain PET imaging of the GluN2B-containing N-methyl-d-aspartate receptor with (R)-11C-Me-NB1
The N-methyl-d-aspartate receptor (NMDAR) plays a crucial role in neurodegenerative
diseases such as Alzheimer disease and in the treatment of major depression by fast-acting …
diseases such as Alzheimer disease and in the treatment of major depression by fast-acting …
Synthesis and Biological Evaluation of Enantiomerically Pure (R)- and (S)-[18F]OF-NB1 for Imaging the GluN2B Subunit-Containing NMDA Receptors
M Korff, A Chaudhary, Y Li, X Zhou… - Journal of Medicinal …, 2023 - ACS Publications
GluN2B subunit-containing N-methyl-d-aspartate (NMDA) receptors have been implicated in
various neurological disorders. Nonetheless, a validated fluorine-18 labeled positron …
various neurological disorders. Nonetheless, a validated fluorine-18 labeled positron …
Evaluation of 11C-Me-NB1 as a potential PET radioligand for measuring GluN2B-containing NMDA receptors, drug occupancy, and receptor cross talk
Clinical and preclinical research with modulators at the N-methyl-d-aspartate (NMDA)
receptor GluN2B N-terminal domain (NTD) aims for the treatment of various neurologic …
receptor GluN2B N-terminal domain (NTD) aims for the treatment of various neurologic …
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