Dataset Information

Instantaneous Conversion of [¹¹ C]CO₂ to [¹¹ C]CO via Fluoride-Activated Disilane Species.

ABSTRACT: The development of a fast and novel methodology to generate carbon-11 carbon monoxide ([¹¹ C]CO) from cyclotron-produced carbon-11 carbon dioxide ([¹¹ C]CO₂ ) mediated by a fluoride-activated disilane species is described. This methodology allows up to 74?% conversion of [¹¹ C]CO₂ to [¹¹ C]CO using commercially available reagents, readily available laboratory equipment and mild reaction conditions (room temperature). As proof of utility, radiochemically pure [carbonyl-¹¹ C]N-benzylbenzamide was successfully synthesized from produced [¹¹ C]CO in up to 74?% radiochemical yield (RCY) and >99?% radiochemical purity (RCP) in ?10?min from end of [¹¹ C]CO₂ delivery.

SUBMITTER: Taddei C

PROVIDER: S-EPMC5488231 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Instantaneous Conversion of [11 C]CO2 to [11 C]CO via Fluoride-Activated Disilane Species.

Taddei Carlotta C Bongarzone Salvatore S Gee Antony D AD

Chemistry (Weinheim an der Bergstrasse, Germany) 20170517 32

The development of a fast and novel methodology to generate carbon-11 carbon monoxide ([11 C]CO) from cyclotron-produced carbon-11 carbon dioxide ([11 C]CO2 ) mediated by a fluoride-activated disilane species is described. This methodology allows up to 74 % conversion of [11 C]CO2 to [11 C]CO using commercially available reagents, readily available laboratory equipment and mild reaction conditions (room temperature). As proof of u ...[more]

PMID: 28419627

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Project description:BackgroundThe ?-amyloid radiotracer [11C] PiB is extensively used for the Positron Emission Tomography (PET) diagnosis of Alzheimer's Disease and related dementias. For clinical use, [11C] PiB is produced using the 11C-methylation method ([11C] Methyl iodide or [11C] methyl triflate as 11C-methylation agents), which represents the most employed 11C-labelling strategy for the synthesis of 11C-radiopharmaceuticals. Recently, the use of direct [11C]CO2 fixation for the syntheses of 11C-tracers has gained interest in the radiochemical community due to its importance in terms of radiochemical versatility and for permitting the direct employment of the cyclotron-produced precursor [11C]CO2. This paper presents an optimised alternative one-pot methodology of [11C]CO2 fixation-reduction for the rapid synthesis of [11C] PiB using an automated commercial platform and its quality control.Results[11C] PiB was obtained from a (25.9?±?13.2)% (Average?±?Variation Coefficient, n?=?3) (end of synthesis, decay corrected) radiochemical yield from trapped [11C]CO2 after 1?min of labelling time using PhSiH3 / TBAF as the fixation-reduction system in Diglyme at 150?°C. The radiochemical purity was higher than 95% in all cases, and the molar activity was (61.4?±?1.6) GBq/?mol. The radiochemical yield and activity (EOS) of formulated [11C] PiB from cyclotron-produced [11C]CO2 was (14.8?±?12.1)%, decay corrected) and 9.88?GBq (± 6.0%), respectively. These are higher values compared to that of the 11C-methylation method with [11C]CH3OTf (~?8.3%).ConclusionsThe viability of the system PhSiH3 / TBAF to efficiently promote the radiosynthesis of [11C] PiB via direct [11C]CO2 fixation-reduction has been demonstrated. [11C] PiB was obtained through a fully automated radiosynthesis with a satisfactory yield, purity and molar activity. According to the results, the one-pot methodology employed could reliably yield sufficiently high tracer amounts for preclinical and clinical use.

Project description:Regenerative medicine-based approaches for caries treatment focus on biomimetic remineralization of initial carious lesions as a minimal invasive therapy. In vitro, self-assembling peptide P11-4 enhances remineralization of early carious lesions. To investigate the safety and clinical efficacy of P11-4 for treatment of initial caries, a randomized controlled single-blind study was conducted on children aged >5 y with visible active early caries on erupting permanent molars. Subjects were randomized to either the test group (P11-4 + fluoride varnish) or control group (fluoride varnish alone). Caries were assessed at baseline and at 3 and 6 mo posttreatment per laser fluorescence, a visual analog scale, the International Caries Detection and Assessment System, and Nyvad caries activity criteria. Intention-to-treat analyses were performed, and safety and clinical feasibility of the treatment approaches were assessed. Compared with the control group, the test group showed clinically and statistically significant improvement in all outcomes at 3 and 6 mo. The laser fluorescence readings (odds ratio = 3.5, P = 0.015) and visual analog scale scores (odds ratio = 7.9, P < .0001) were significantly lower for the test group, and they showed regression in the International Caries Detection and Assessment System caries index (odds ratio = 5.1, P = 0.018) and conversion from active to inactive lesions according to Nyvad criteria (odds ratio = 12.2, P < 0.0001). No adverse events occurred. The biomimetic mineralization facilitated by P11-4 in combination with fluoride application is a simple, safe, and effective noninvasive treatment for early carious lesions that is superior to the presently used gold standard of fluoride alone. By regenerating enamel tissue and preventing lesion progression, this novel approach could change clinical dental practice from a restorative to a therapeutic approach. This could avoid additional loss of healthy hard tissue during invasive restorative treatments, potentially enabling longer tooth life and thereby lowering long-term health costs ( ClinicalTrials.gov NCT02724592).

Dataset Information

Instantaneous Conversion of [¹¹ C]CO₂ to [¹¹ C]CO via Fluoride-Activated Disilane Species.

Publications

Instantaneous Conversion of [<sup>11</sup> C]CO<sub>2</sub> to [<sup>11</sup> C]CO via Fluoride-Activated Disilane Species.

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