Novel ¹⁸F-Labeled PET Imaging Agent FV45 Targeting the Renin-Angiotensin System.

ABSTRACT: Renin-angiotensin system (RAS) plays an important role in the regulation of blood pressure and hormonal balance. Using positron emission tomography (PET) technology, it is possible to monitor the physiological and pathological distribution of angiotensin II type 1 receptors (AT₁), which reflects the functionality of RAS. A new ¹⁸F-labeled PET tracer derived from the clinically used AT₁ antagonist valsartan showing the least possible chemical alteration from the valsartan structure has been designed and synthesized with several strategies, which can be applied for the syntheses of further derivatives. Radioligand binding study showed that the cold reference FV45 (K _i 14.6 nM) has almost equivalent binding affinity as its lead valsartan (

SUBMITTER: Chen X 

PROVIDER: S-EPMC6166228 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature