Automated two-step manufacturing of [11C]glyburide radiopharmaceutical for PET imaging in humans

[11C]glyburide PET imaging for quantitative determination of the importance of Organic Anion-Transporting Polypeptide transporter function in the human liver and whole-body

“…[ 11 C]glyburide was synthesized using a previously described automated two-step method [31]. Detailed information are provided as Supplementary data.…”

“…Isotopic radiolabeling of glyburide with carbon-11 ([ 11 C]glyburide) is feasible [31]. [ 11 C]glyburide PET imaging was therefore evaluated in healthy volunteers as a probe for OATP function.…”

Radiolabeling and brain penetration of [11C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging

“…8,9 The sulfonylurea drug glyburide benefits from high affinity for SUR1 10 and radiolabeling of glyburide with carbon-11 for clinical PET imaging has been reported. 11 However, [ 11 C]glyburide poorly crosses the intact blood-brain barrier (BBB) in animals 12 and humans. 13 There is therefore a need for CNS-penetrant ligands of SUR1 to explore this biomarker using brain PET.…”

“…Radiochemistry4.2.1 | Optimization of the radiomethylation stepAutomated radiosynthesis with carbon-11 was performed using a TRACERlab ® FX C Pro module (GE Healthcare, GBq) was produced via the 14 N(p, α)11 C nuclear reaction by irradiation of a [ 14 N]N 2 target containing 0.15-0.5% of O 2 on a cyclone 18/9 cyclotron (18 MeV, IBA, Belgium). [ 11 C]CO 2 was subsequently reduced to [ 11 C]CH 4 and iodinated to [ 11 C]CH 3 I following the process described by Larsen et al17 For one experiment, [ 11 C]CH 3 I was converted into [ 11 C]CH 3 OTf according to the method of Jewett.…”

Interrupted Aza-Wittig Reactions Using Iminophosphoranes to Synthesize 11C-Carbonyls

“…31 [ 11 C]Glibenclamide ([ 11 C]36) is a substrate for organic anion-transportingpolypeptide (OATP) transporter and can be used to study the integrity of the blood-brain barrier by non-invasive PET imaging 32,33. This radiopharmaceutical, which is currently synthesized in two-steps using [ 11 C]CH3OTf, was efficiently labeled using an iminophosphorane precursor directly from [ 11 C]CO2 34. Following purification 7.4 ± 1.9 GBq of [ 11 C]glibenclamide was obtained with an isolated decay corrected yield of 62 ± 16% from 25.9 GBq of [ 11 C]CO2, and a molar activity of 59 ± 0.06 GBq•µmol -1 within 21 minutes from the beginning of synthesis.…”