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Selective Radioligand (selective + radioligand)
Selected AbstractsDevelopment of an Efficient and Selective Radioligand for Bradykinin B1 Receptor Occupancy Studies.CHEMINFORM, Issue 16 2005Dai-Shi Su Abstract For Abstract see ChemInform Abstract in Full Text. [source] Efficient synthesis of [11C]befloxatone, a selective radioligand for the in vivo imaging of MAO-A density using PETJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 9 2003F. Dollé Abstract Carbon-11 labelled befloxatone ((5R)-5-(methoxymethyl)-3-[4-[(3R)-4,4,4-trifluoro-3-hydroxybutoxy]phenyl]-2-oxazolidinone) is a reversible and selective monoamine oxidase-A (MAO-A) inhibitor and appears to be a new potent PET tracer for the in vivo imaging of MAO-A density. In this paper, the radiosynthesis of befloxatone was investigated and orientated towards the preparation of multi milliCuries of radiotracer. Typically, using no-carrier-added [11C]phosgene, 150,300 mCi (5.55,11.10 GBq) of [11C]befloxatone was obtained within 20 min of radiosynthesis (including HPLC purification) with specific radioactivities ranging from 500 to 2000 mCi/µmol (18.5,74.0 GBq/µmol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer. Copyright © 2003 John Wiley & Sons, Ltd. [source] Efficient synthesis and formulation of (R)-(,)-[11C]Deprenyl, a selective radioligand for the quantification of MAO-B activity using PETJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 10 2002Frédéric Dolle Abstract Carbon-11 labeled (R)-(,)-Deprenyl is the tracer of reference for the quantification of monoamine oxidase (MAO)-B activity with PET. In this paper, its radiosynthesis is re-investigated and oriented towards the preparation of multi-milliCuries of radiotracer. Typically, using no-carrier-added [11C]methyl triflate as the alkylating agent, 140,190 mCi (5.1,7.0 GBq) of (R)-(,)-[11C]Deprenyl was obtained within 30 min of radiosynthesis (including HPLC purification and formulation) with specific radioactivities ranging from 0.8 to 1.2 Ci/,mol (29.6,44.4 GBq/,mol). The high efficiency of these radiosyntheses allows for multi-injection protocols and kinetic approaches for absolute quantification of the tracer. Copyright © 2002 John Wiley & Sons, Ltd. [source] Precursor synthesis and radiolabelling of [11C]ADAM: a potential radioligand for the serotonin transporter exploration by PETJOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 2 2001Johnny VERCOUILLIE Abstract The serotoninergic system is involved in a variety of neurological and psychiatric disorders. Exploration of the serotonin transporters (5-HTT) in living human brain by PET would be of great value for better understanding, diagnosis and therapeutic follow up of these diseases. In order to obtain a selective radioligand to explore the 5-HTT by PET we report the synthesis of [11C]N,N-dimethyl-2-(2-amino-4-iodophenylthio)-benzylamine ([11C]ADAM). The precursor for labelling N-demethyl ADAM, was obtained in five steps using 2,5-dibromonitrobenzene and 2-thio-N-methylbenzamide as starting material. [11C]ADAM was synthesised by N-alkylation of the precursor using [11C]methyl iodide in DMF. The incorporation yield of [11C]methyl iodide was in the range of 50 to 70%. Finally [11C]ADAM was obtained in 30 minutes synthesis time including HPLC and with a radiochemical purity better than 99%. Copyright © 2001 John Wiley & Sons, Ltd. [source] | ||||||||||