Comment on ' In Vivo [18F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates'
| Autor: | Jonathan P. Coles, Matthias J. Koepp, Colm J. McGinnity, Ella Hirani, Erik Årstad, Nisha Singh, Marian Galovic, Paul A. Jones, William Trigg, Alexander Hammers, David J. Brooks, Feng Luo, Rainer Hinz, Daniela A. Riaño Barros, Oliver D. Howes, Katherine Beck, John S. Duncan |
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| Přispěvatelé: | McGinnity, Colm J [0000-0002-2692-918X], Årstad, Erik [0000-0002-3240-2106], Apollo - University of Cambridge Repository |
| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Drug
N-Methylaspartate Physiology Cognitive Neuroscience media_common.quotation_subject Rodentia Biochemistry 03 medical and health sciences 0302 clinical medicine In vivo medicine Animals Inhibitory effect 030304 developmental biology media_common 0303 health sciences Chemistry Glutamate receptor Brain Cell Biology General Medicine Macaca mulatta Rats Isoflurane Positron-Emission Tomography NMDA receptor Radiopharmaceuticals Neuroscience 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | McGinnity, C J, Årstad, E, Beck, K, Brooks, D J, Coles, J P, Duncan, J S, Galovic, M, Hinz, R, Hirani, E, Howes, O D, Jones, P A, Koepp, M J, Luo, F, Riaño Barros, D A, Singh, N, Trigg, W & Hammers, A 2019, ' Comment on " In Vivo [18F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates" ', ACS Chemical Neuroscience, vol. 10, no. 1, pp. 768-772 . https://doi.org/10.1021/acschemneuro.8b00246 Mcginnity, C J, Årstad, E, Beck, K, Brooks, D J, Coles, J P, Duncan, J S, Galovic, M, Hinz, R, Hirani, E, Howes, O D, Jones, P A, Koepp, M J, Luo, F, Riaño Barros, D A, Singh, N, Trigg, W & Hammers, A 2018, ' Comment on “In Vivo [18 F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates” ', ACS Chemical Neuroscience . https://doi.org/10.1021/acschemneuro.8b00246 |
| Popis: | Schoenberger and colleagues ( Schoenberger et al. ( 2018 ) ACS Chem. Neurosci. 9 , 298 - 305 ) recently reported attempts to demonstrate specific binding of the positron emission tomography (PET) radiotracer, [18F]GE-179, to NMDA receptors in both rats and Rhesus macaques. GE-179 did not work as expected in animal models; however, we disagree with the authors' conclusion that "the [18F]GE-179 signal seems to be largely nonspecific". It is extremely challenging to demonstrate specific binding for the use-dependent NMDA receptor intrachannel ligands such as [18F]GE-179 in animals via traditional blocking, due to its low availability of target sites ( Bmax'). Schoenberger and colleagues anesthetized rats and Rhesus monkeys using isoflurane, which has an inhibitory effect on NMDA receptor function and thus would be expected to further reduce the Bmax'. The extent of glutamate release achieved in the provocation experiments is uncertain, as is whether a significant increase in NMDA receptor channel opening can be expected under anesthesia. Prior data suggest that the uptake of disubstituted arylguanidine-based ligands such as GE-179 can be reduced by phencyclidine binding site antagonists, if injection is performed in the absence of ketamine and isoflurane anesthesia, e.g., with GE-179's antecedent, CNS 5161 ( Biegon et al. ( 2007 ) Synapse 61 , 577 - 586 ), and with GMOM ( van der Doef et al. ( 2016 ) J. Cereb. Blood Flow Metab. 36 , 1111 - 1121 ). However, the extent of nonspecific uptake remains uncertain. |
| Databáze: | OpenAIRE |
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