Preclinical evaluation of carbon-11 and fluorine-18 sulfonamide derivatives for in vivo radiolabeling of erythrocytes.

ABSTRACT:

Unlabelled

Background

To date, few PET tracers for in vivo labeling of red blood cells (RBCs) are available. In this study, we report the radiosynthesis and in vitro and in vivo evaluation of 11C and 18F sulfonamide derivatives targeting carbonic anhydrase II (CA II), a metallo-enzyme expressed in RBCs, as potential blood pool tracers. A proof-of-concept in vivo imaging study was performed to demonstrate the feasibility to assess cardiac function and volumes using electrocardiogram (ECG)-gated positron emission tomography (PET) acquisition in comparison with cine magnetic resonance imaging (cMRI) in rats and a pig model of myocardial infarction.

Methods

The inhibition constants (Ki) of CA II were determined in vitro for the different compounds by assaying CA-catalyze

SUBMITTER: Gheysens O 

PROVIDER: S-EPMC3561128 | biostudies-literature | 2013 Jan

REPOSITORIES: biostudies-literature