Radiolabeling and brain penetration of [11 C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging.
J Labelled Comp Radiopharm
; 65(2): 28-35, 2022 02.
Article
em En
| MEDLINE
| ID: mdl-34796549
ABSTRACT
Sulfonylurea receptor 1 (SUR1) overexpression in the central nervous system is a potential biomarker for positron emission tomography (PET) imaging of brain damage and recovery. VU0071063, a selective ligand of SUR1 able to cross the blood-brain barrier, was isotopically radiolabeled with carbon-11 from a desmethyl precursor obtained quantitatively in one step. Ready-to-inject [11C]VU0071063 was obtained in 18 ± 2% radiochemical yield and 103 ± 22 GBq/µmol molar activity. PET imaging in healthy rats demonstrated a significant brain penetration and rapid elimination of the tracer in vivo, encouraging further investigation in animal models of SUR1 overexpression.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Radiofarmacêuticos
/
Tomografia por Emissão de Pósitrons
Limite:
Animals
Idioma:
En
Revista:
J Labelled Comp Radiopharm
Ano de publicação:
2022
Tipo de documento:
Article
País de afiliação:
França