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Improved syntheses of P2X7 ligands based on substituted benzyl amide of pyroglutamic acid motif labelled with iodine-123 or iodine-125.
- Source :
-
Journal of Radioanalytical & Nuclear Chemistry . Oct2023, Vol. 332 Issue 10, p4191-4199. 9p. 1 Color Photograph, 4 Diagrams, 1 Chart, 1 Graph. - Publication Year :
- 2023
-
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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 02365731
- Volume :
- 332
- Issue :
- 10
- Database :
- Academic Search Index
- Journal :
- Journal of Radioanalytical & Nuclear Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 172867434
- Full Text :
- https://doi.org/10.1007/s10967-023-09081-2