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Mol Imaging Biol. 2012 Oct;14(5):625-36.

Structure--activity relationship and preclinical evaluation of carbon-11-labeled ammonium salts as PET--myocardial perfusion imaging agents.

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1
Cyclotron/Radiochemistry Unit/Nuclear Medicine Department, Hadassah Hebrew University Hospital, Jerusalem, 91120, Israel.

Abstract

BACKGROUND:

Due to the limited availability of suitable positron emission tomography (PET) tracers, the majority of myocardial perfusion imaging (MPI) scans is performed using SPECT rather than PET.

AIM:

The aim of this study is to design and synthesize carbon-11-labeled ammonium salt derivatives and explore their structure–activity relationship (SAR) and their potential as PET–MPI agents.

METHODS AND RESULTS:

Three carbon-11-labeled ammonium salts were developed. SAR of the labeled compounds were explored vis-à-vis the effects of charge density and lipophilicity on the distribution kinetics in mice. These studies pointed at [11C]4 as the lead compound. Comparative microPET/CT scans in healthy rats, using both [11C]4 and [13 N]–NH3, substantiated the potential of [11C]4 ([11C]-DMDPA). A proof of concept for the potential of radiolabeled ammonium salts as MPI agents has been demonstrated in a newly developed swine model of permanent partial coronary artery occlusion.

CONCLUSIONS:

SAR studies of 11C-labeled ammonium salts suggest that both lipophilicity and charge density affect the performance of these compounds as MPI probes. In a swine model, the labeled lead successfully visualized the defect regions in the myocardium. The data presented call for the development of fluorine-18 analogues, to increase clinical impact.

PMID:
22290562
DOI:
10.1007/s11307-011-0539-6
[Indexed for MEDLINE]
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