2017
DOI: 10.1038/srep42136
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Imaging cardiac SCN5A using the novel F-18 radiotracer radiocaine

Abstract: The key function of the heart, a well-orchestrated series of contractions, is controlled by cardiac action potentials. These action potentials are initiated and propagated by a single isoform of voltage gated sodium channels – SCN5A. However, linking changes in SCN5A expression levels to human disease in vivo has not yet been possible. Radiocaine, an F-18 radiotracer for positron emission tomography (PET), is the first SCN5A imaging agent in the heart. Explants from healthy and failing human hearts were compar… Show more

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Cited by 8 publications
(13 citation statements)
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“…[ 18 F]­GE-179 was synthesized using a thiophenol precursor purchased from GE Healthcare (Amersham, UK) for [ 18 F]­fluoroethylation as previously described . Briefly, the radionuclide 18 F and the common alkylation building block [ 18 F]­fluoroethyl tosylate (FETs) were synthesized as described earlier in our lab . Freshly prepared FETs was added to 0.8 mg of precursor and 0.5 mg of K 2 CO 3 as a solution in 0.5 mL of acetonitrile.…”
Section: Methodsmentioning
confidence: 99%
“…[ 18 F]­GE-179 was synthesized using a thiophenol precursor purchased from GE Healthcare (Amersham, UK) for [ 18 F]­fluoroethylation as previously described . Briefly, the radionuclide 18 F and the common alkylation building block [ 18 F]­fluoroethyl tosylate (FETs) were synthesized as described earlier in our lab . Freshly prepared FETs was added to 0.8 mg of precursor and 0.5 mg of K 2 CO 3 as a solution in 0.5 mL of acetonitrile.…”
Section: Methodsmentioning
confidence: 99%
“…In both cases, specific binding could be characterized successfully by traditional in vivo competition experiments. 13 These experimental data demonstrate that PET imaging probes that act as activity-dependent ion channel pore blockers, as is the case for [ 18 F]GE-179, are amenable to presaturation, competition, and chase-experiments.…”
mentioning
confidence: 74%
“…However, it is important to point out that other activity-dependent binders, e.g., a local anesthetic and a dihydropyridine, have been used as PET imaging probes for voltage gated sodium and calcium channels, respectively. , The respective binding sites of these probes are structurally related to NMDA receptors. In both cases, specific binding could be characterized successfully by traditional in vivo competition experiments . These experimental data demonstrate that PET imaging probes that act as activity-dependent ion channel pore blockers, as is the case for [ 18 F]­GE-179, are amenable to presaturation, competition, and chase-experiments.…”
mentioning
confidence: 81%
“…Notably, this radiolabeling approach is complementary to Hooker's synthesis of the 18 F-fluoroethyl analogue [ 18 F]radiocaine. 54 Protected aromatic amino acid derivatives undergo high yielding radiofluorination to afford products such as 18-18 F and 19-18 F. These have potential applications for imaging dopaminergic metabolism and tumor proliferation. 55 Automated labeling was followed by semipreparative HPLC purification to afford 18-18 F in 25% isolated RCY, 99% RCP, and 0.52 Ci/μmol (19.24 GBq/μmol) A m (n = 2).…”
Section: ■ Results and Discussionmentioning
confidence: 99%
“…Under the standard C–H borylation/CMRF conditions, the anesthetic lidocaine reacts to furnish 17- 18 F in 15 ± 8% RCY. Notably, this radiolabeling approach is complementary to Hooker’s synthesis of the 18 F-fluoroethyl analogue [ 18 F]­radiocaine …”
Section: Resultsmentioning
confidence: 99%