Please use this identifier to cite or link to this item:
http://dx.doi.org/10.25673/115216
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DC Field | Value | Language |
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dc.contributor.author | Chen, Jiahui | - |
dc.contributor.author | Ran, Wenqing | - |
dc.contributor.author | Huang, Yiman | - |
dc.contributor.author | Wei, Junjie | - |
dc.contributor.author | Rong, Jian | - |
dc.contributor.author | Wei, Huiyi | - |
dc.contributor.author | Li, Yinlong | - |
dc.contributor.author | Li, Guocong | - |
dc.contributor.author | Chen, Zhen | - |
dc.contributor.author | Collier, Lee | - |
dc.contributor.author | Elghazawy, Nehal H. | - |
dc.contributor.author | Sippl, Wolfgang | - |
dc.contributor.author | Haider, Ahmed | - |
dc.contributor.author | Liao, Kai | - |
dc.contributor.author | Dong, Chenchen | - |
dc.contributor.author | Li, Ying | - |
dc.contributor.author | Xu, Hao | - |
dc.contributor.author | He, Wenpeng | - |
dc.contributor.author | Wang, Lu | - |
dc.contributor.author | Liang, Steven H. | - |
dc.date.accessioned | 2024-03-07T07:53:59Z | - |
dc.date.available | 2024-03-07T07:53:59Z | - |
dc.date.issued | 2023 | - |
dc.identifier.uri | https://opendata.uni-halle.de//handle/1981185920/117172 | - |
dc.identifier.uri | http://dx.doi.org/10.25673/115216 | - |
dc.description.abstract | As a subclass of ionotropic glutamate receptors (iGluRs), α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptors have been implicated in various neurological disorders and neurodegenerative diseases. To further our understanding of AMPA receptor-related disorders in the central nervous system (CNS), it is important to be able to image and quantify AMPA receptors in vivo. In this study, we identified a novel F-containing AMPA positive allosteric modulator (PAM) 6 as a potential lead compound. Molecular docking studies and CNS PET multi-parameter optimization (MPO) analysis were used to predict the absorption, distribution, metabolism, and excretion (ADME) characteristics of 6 as a PET probe. The resulting PET probe, [18F]6 (codename [18F]AMPA-2109), was successfully radiolabeled and demonstrated excellent blood-brain barrier (BBB) permeability and high brain uptake in rodents and non-human primates. However, [18F]6 did not show substantial specific binding in the rodent or non-human primate brain. Further medicinal chemistry efforts are necessary to improve specific binding, and our work may serve as a starting point for the design of novel 18F-labeled AMPA receptor-targeted PET radioligands aimed for clinical translation. | eng |
dc.language.iso | eng | - |
dc.rights.uri | https://creativecommons.org/licenses/by-nc-nd/4.0/ | - |
dc.subject.ddc | 615 | - |
dc.title | Evaluation of thiadiazine-based PET radioligands for imaging the AMPA receptor | eng |
dc.type | Article | - |
local.versionType | publishedVersion | - |
local.bibliographicCitation.journaltitle | Biomedicine & pharmacotherapy | - |
local.bibliographicCitation.volume | 168 | - |
local.bibliographicCitation.publishername | Elsevier Science | - |
local.bibliographicCitation.publisherplace | Amsterdam [u.a.] | - |
local.bibliographicCitation.doi | 10.1016/j.biopha.2023.115842 | - |
local.subject.keywords | AMPA receptors, central nervous system (CNS), positron emission tomography, positive allosteric modulator (PAM), fluorine 18 (18F) | - |
local.openaccess | true | - |
dc.identifier.ppn | 187307414X | - |
cbs.publication.displayform | 2023 | - |
local.bibliographicCitation.year | 2023 | - |
cbs.sru.importDate | 2024-03-07T07:53:26Z | - |
local.bibliographicCitation | Enthalten in Biomedicine & pharmacotherapy - Amsterdam [u.a.] : Elsevier Science, 1989 | - |
local.accessrights.dnb | free | - |
Appears in Collections: | Open Access Publikationen der MLU |
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1-s2.0-S0753332223016402-main.pdf | 6.4 MB | Adobe PDF | ![]() View/Open |