Preclinical Evaluations of Cardiac Sympathetic Innervation Radiotracers

Raffel, David M.

doi:10.1007/978-3-662-45074-1_10

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“…For (c), the guanidine group of the side chain of [ 18 F] 1 and [ 18 F] 2 confers stability against neuronal enzymes such as tyrosine hydroxylase, MAO, dopamine-β-hydroxylase, or DOPA decarboxylase . Previous studies with the carbon-11 analog of [ 18 F] 1 in rats showed that 100% of the activity in the myocardium at t = 30 min after tracer administration was in the form of the parent tracer, consistent with no intraneuronal metabolism of the tracer . Thus, [ 18 F] 1 and [ 18 F] 2 have been found to satisfy all of our targeted neuronal tracer properties.…”

Section: Results and Discussionmentioning

confidence: 92%

“…32 Previous studies with the carbon-11 analog of [ 18 F]1 in rats showed that 100% of the activity in the myocardium at t = 30 min after tracer administration was in the form of the parent tracer, consistent with no intraneuronal metabolism of the tracer. 33 Thus, [ 18 F]1 and [ 18 F]2 have been found to satisfy all of our targeted neuronal tracer properties.…”

Section: ■ Results and Discussionmentioning

confidence: 93%

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[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

Jung

Jang

et al. 2017

ACS Chem. Neurosci.

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Fluorine-18 labeled phenethylguanidines are currently under development in our laboratory as radiotracers for quantifying regional cardiac sympathetic nerve density using PET imaging techniques. In this study, we report an efficient synthesis of 18F-hydroxyphenethylguanidines consisting of nucleophilic aromatic [18F]fluorination of a protected diaryliodonium salt precursor followed by a single deprotection step to afford the desired radiolabeled compound. This approach has been shown to reliably produce 4-[18F]fluoro-m-hydroxyphenethylguanidine ([18F]4F-MHPG, [18F]1) and its structural isomer 3-[18F]fluoro-p-hydroxyphenethylguanidine ([18F]3F-PHPG, [18F]2) with good radiochemical yields. Preclinical evaluations of [18F]2 in non-human primates were performed to compare its imaging properties, metabolism, and myocardial kinetics with those obtained previously with [18F]1. The results of these studies have demonstrated that [18F]2 exhibits imaging properties comparable to those of [18F]1. Myocardial tracer kinetic analysis of each tracer provides quantitative metrics of cardiac sympathetic nerve density. Based on these findings, first-in-human PET studies with [18F]1 and [18F]2 are currently in progress to assess their ability to accurately measure regional cardiac sympathetic denervation in patients with heart disease, with the ultimate goal of selecting a lead compound for further clinical development.

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Section: Results and Discussionmentioning

confidence: 92%

Section: ■ Results and Discussionmentioning

confidence: 93%

[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

Jung

Jang

et al. 2017

ACS Chem. Neurosci.

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Preclinical Evaluations of Cardiac Sympathetic Innervation Radiotracers

Cited by 1 publication

References 44 publications

[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

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Preclinical Evaluations of Cardiac Sympathetic Innervation Radiotracers

Cited by 1 publication

References 44 publications

[18F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

[18F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

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[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation

[¹⁸F]Fluoro-Hydroxyphenethylguanidines: Efficient Synthesis and Comparison of Two Structural Isomers as Radiotracers of Cardiac Sympathetic Innervation