Development of 68Ga‐labeled fatty acids for their potential use in cardiac metabolic imaging. (15th June 2014)

• Record Type: Journal Article
• Authors: Jindal, Akanksha; Mathur, Anupam; Pandey, Usha; Sarma, H. D.; Chaudhari, Pradip; Dash, Ashutosh
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 57:Number 7(2014)
• Page Start: 463
• Page End: 469
• Publication Date: 2014-06-15
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3205
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>While [<sup>11</sup>C]palmitate continues to be a promising tracer for cardiovascular Positron Emission Tomography (PET) imaging, unfavourable logistics due to the short half‐life of <sup>11</sup>C (20 min) and cumbersome labeling methodologies are the major impediments that limit its widespread use. In order to circumvent such limitations, an attempt has been made to explore the potential of <sup>68</sup>Ga‐labeled fatty acid analogs for metabolic imaging owing to the availability of <sup>68</sup>Ga through a <sup>68</sup>Ge/<sup>68</sup>Ga generator on an on‐demand basis. In this study, two fatty acid conjugates were synthesized by conjugation of <italic>p</italic>‐SCN‐benzyl NOTA with the <italic>ω</italic>‐amino group of 11‐amino undecanoic acid and 12‐amino dodecanoic acid, respectively, under alkaline conditions. Both derivatives were radiolabeled in high yields with <sup>68</sup>Ga obtained from an in‐house <sup>68</sup>Ge/<sup>68</sup>Ga generator. Biodistribution studies in Swiss mice showed reasonable myocardial uptake at 2 min for both derivatives (7.4 ± 2.8% ID/g for 11‐carbon fatty acid‐NOTA conjugate and 6.4 ± 2.1% ID/g for 12‐carbon fatty acid‐NOTA conjugate), which cleared rapidly over 30 min. However, significant activity was found in blood for both tracers, with heart/blood ratios observed to be below 0.5 at all time points, diminishing the potential of the synthesized complexes for cardiac imaging. Copyright © 2014 John Wiley & Sons, Ltd.</p> </abstract>