http://www.cnr.it/ontology/cnr/individuo/prodotto/ID182910
Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration (Articolo in rivista)
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- Label
- Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration (Articolo in rivista) (literal)
- Anno
- 2004-01-01T00:00:00+01:00 (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
- 10.1016/j.neuint.2003.08.006 (literal)
- Alternative label
S. Belloli a; R.M. Moresco a; M. Matarrese a; G. Biella a; F. Sanvito a; P. Simonelli a;
E. Turolla a; S. Olivieri a; A. Cappelli b; S. Vomero b; M. Galli-Kienle a; F. Fazio a (2004)
Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration
in Neurochemistry international; Pergamon-Elsevier Science Ltd., Oxford (Regno Unito)
(literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- S. Belloli a; R.M. Moresco a; M. Matarrese a; G. Biella a; F. Sanvito a; P. Simonelli a;
E. Turolla a; S. Olivieri a; A. Cappelli b; S. Vomero b; M. Galli-Kienle a; F. Fazio a (literal)
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- Note
- ISI Web of Science (WOS) (literal)
- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
- a IBFM-CNR, University of Milan-Bicocca, H. San Raffaele, 20132 Milan, Italy
b University of Siena, Italy (literal)
- Titolo
- Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration (literal)
- Abstract
- The peripheral-type benzodiazepine receptors (PBRs) are only minimally expressed in normal brain parenchyma, where they are
primarily localized in glial cells. Their basal expression rises in different neurodegenerative disorders, due to the presence of infiltrating
inflammatory cells and activated microglia. [11C]PK11195, a selective PBR antagonist, has been used for the in vivo PET monitoring
of neurodegeneration in clinical observations. We recently developed and labeled with carbon-11 three new carboxamide derivatives:
[11C]VC193M, [11C]VC195 and [11C]VC198M. Aim of this study was to evaluate these ligands for the in vivo measuring of PBRs
expression in neurodegenerations and compare their kinetic behavior with that of the reference tracer [11C]PK11195. Radioligands were
evaluated in a preclinical model of Huntington's disease consisting in the monolateral striatal injection of quinolinic acid (QA). Activated
microglia and astrocytic gliosis was present only within the affected striatum. A concomitant increase in radioactivity accumulation was
observed for all the tracers examined (P < 0.01). Among the new compounds, [11C]VC195 showed higher levels of lesioned/unlesioned
striatum ratios (3.28±0.44), in comparison with [11C]VC193M and [11C]VC198M (2.69±0.53 and 1.52±0.36, respectively), but slightly
inferior to that observed for [11C]PK11195 (3.76 ± 1.41).
In conclusion, the results of the study indicate that [11C]VC195 is a promising candidate for in vivo PET monitoring of neurodegenerative
processes but its in vivo behavior overlap that of [11C]PK11195. (literal)
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