Radiosynthesis of 2-[6-chloro-2-(4-iodophenyl)imidazo [1,2-a]pyridin-3-yl]-N-ethyl-N-[C-11]methyl-acetamide, [C-11]CLINME, a novel radioligand for imaging the peripheral benzodiazepine receptors with PET

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dc.contributor.authorThominiaux, CJen_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorGreguric, Ien_AU
dc.contributor.authorBoutin, Hen_AU
dc.contributor.authorChauveau, Fen_AU
dc.contributor.authorKuhnast, Ben_AU
dc.contributor.authorGrégoire, MCen_AU
dc.contributor.authorLoc'h, Cen_AU
dc.contributor.authorValette, Hen_AU
dc.contributor.authorBottlaender, MAen_AU
dc.contributor.authorHantraye, Pen_AU
dc.contributor.authorTavitian, Ben_AU
dc.contributor.authorKatsifis, Aen_AU
dc.contributor.authorDollé, Fen_AU
dc.date.accessioned2009-06-11T03:53:34Zen_AU
dc.date.accessioned2010-04-30T05:06:53Zen_AU
dc.date.available2009-06-11T03:53:34Zen_AU
dc.date.available2010-04-30T05:06:53Zen_AU
dc.date.issued2007-03en_AU
dc.date.statistics2007-03en_AU
dc.description.abstractRecently, a new 2-(iodophenyl)imidazo[1,2-a]pyridineacetamide series has been developed as iodine-123-labelled radioligands for imaging the peripheral benzodiazepine receptors using single photon emission tomography. Within this series, 2-[6-chloro-2-(4-iodophenyl)-imidazo[1,2-alpyridin-3-yl]-N-ethyl-N-methyl-acetamide (CLINME) was considered as an appropriate candidate for positron emission tomography imaging and was isotopically labelled with carbon-11 (T-1/2: 20.38 min) at the methylacetamide side chain from the corresponding nor-analogue using [C-11]methyl iodide and the following experimental conditions: (1) trapping at -10 degrees C of [C-11]methyl iodide in a 1/2 (v:v) mixture of DMSO/DMF (300 mu l) containing 0.7-1.0 mg of the precursor for labelling and 3-5 mg of powdered potassium hydroxide (excess); (2) heating the reaction mixture at 110 degrees C for 3 min under a nitrogen stream; (3) diluting the residue with 0.6 ml of the HPLC mobile phase; and (4) purification using semi-preparative HPLC (Zorbax(R) SB18, Hewlett Packard, 250 x 9.4 mm). Typically, starting from a 1.5Ci (55.5 GBq) [C-11]CO2 production batch, 120-150 mCi (4.44-5.55 GBq) of [C-11]CLINME were obtained (16-23% decay-corrected radiochemical yield, n = 12) within a total synthesis time of 24-27 min (Sep-pak(R)Plus-based formulation included). Specific radio-activities ranged from 0.9 to 2.7 Ci/mu mol (33.3-99.9 GBq/mu mol) at the end of radiosynthesis. © 2007, Wiley-Blackwell.en_AU
dc.identifier.citationThominiaux, C., Mattner, F., Greguric, I., Boutin, H., Chauveau, F., Kuhnast, B.,Grégoire , M. C., Loc'h, C., Valette, H., Bottlaender, M. A., Hantraye, P., Tavitian, B., Katsifis, A., & Dollé, F. (2007). Radiosynthesis of 2-[6-chloro-2-(4-iodophenyl)imidazo [1,2-a]pyridin-3-yl]-N-ethyl-N-[C-11]methyl-acetamide, [C-11]CLINME, a novel radioligand for imaging the peripheral benzodiazepine receptors with PET. Journal of Labelled Compounds and Radiopharmaceuticals, 50(3-4), 229-236. doi:10.1002/jlcr.1258en_AU
dc.identifier.govdoc1440en_AU
dc.identifier.issn0362-4803en_AU
dc.identifier.issue3-4en_AU
dc.identifier.journaltitleJournal of Labelled Compounds and Radiopharmaceuticalsen_AU
dc.identifier.pagination229-236en_AU
dc.identifier.urihttp://dx.doi.org/10.1002/jlcr.1258en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/1333en_AU
dc.identifier.volume50en_AU
dc.language.isoenen_AU
dc.publisherWiley-Blackwellen_AU
dc.subjectLigandsen_AU
dc.subjectReceptorsen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectSingle photon emission computed tomographyen_AU
dc.subjectSynthesisen_AU
dc.subjectLabelled compoundsen_AU
dc.titleRadiosynthesis of 2-[6-chloro-2-(4-iodophenyl)imidazo [1,2-a]pyridin-3-yl]-N-ethyl-N-[C-11]methyl-acetamide, [C-11]CLINME, a novel radioligand for imaging the peripheral benzodiazepine receptors with PETen_AU
dc.typeJournal Articleen_AU
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