Improved syntheses of P2X7 ligands based on substituted benzyl amide of pyroglutamic acid motif labelled with iodine-123 or iodine-125
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F23%3A73619791" target="_blank" >RIV/61989592:15110/23:73619791 - isvavai.cz</a>
Alternative codes found
RIV/61989592:15640/23:73619791 RIV/60461373:22330/23:43926721
Result on the web
<a href="https://link.springer.com/article/10.1007/s10967-023-09081-2" target="_blank" >https://link.springer.com/article/10.1007/s10967-023-09081-2</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s10967-023-09081-2" target="_blank" >10.1007/s10967-023-09081-2</a>
Alternative languages
Result language
angličtina
Original language name
Improved syntheses of P2X7 ligands based on substituted benzyl amide of pyroglutamic acid motif labelled with iodine-123 or iodine-125
Original language description
Abstract: P2X7 sites are emerging targets for molecular imaging research, notably in the context of neurodegeneration and inflammatory conditions. Therefore, we prepared a precursor for (radio)iodination of the P2X7 ligand VPGIS191. We then developed a radioiodination method with 123I for SPECT with a radiochemical yield of 71 ± 13% and 125I for autoradiography with a radiochemical yield of 85 ± 6% Autoradiography of [125I]VPGIS191 in mouse brain cryostat sections demonstrated approximately 36 nM binding affinity and Bmax of approximately 400 pmol/gram tissue for P2X7 binding sites. VPGIS191 (cis) had a two-fold lower affinity compared to its geometric trans-isomer TZ6019.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10406 - Analytical chemistry
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2023
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
ISSN
0236-5731
e-ISSN
1588-2780
Volume of the periodical
332
Issue of the periodical within the volume
10
Country of publishing house
HU - HUNGARY
Number of pages
9
Pages from-to
4191-4199
UT code for WoS article
001049812700002
EID of the result in the Scopus database
2-s2.0-85168083105