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Synthesis of [ 11 C]granisetron, a possible positron emission tomography ligand for 5‐HT3 receptor studies
Author(s) -
Vandersteene I.,
Audenaert K.,
Slegers G.,
Dierckx R.
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199803)41:3<171::aid-jlcr66>3.0.co;2-f
Subject(s) - chemistry , radioligand , granisetron , desmethyl , methyl iodide , radiosynthesis , high performance liquid chromatography , positron emission tomography , radiochemistry , labelling , ligand (biochemistry) , radioligand assay , specific activity , antagonist , iodide , chromatography , receptor , nuclear medicine , medicinal chemistry , organic chemistry , metabolite , biochemistry , medicine , antiemetic , vomiting , enzyme
[ 11 C]Granisetron, a selective 5‐HT3 antagonist, was synthesized by N‐alkylation of the desmethyl compound using [ 11 C]methyl iodide as the labelling agent in a total synthesis time of 40 min, including semi‐preparative HPLC purification. Approximately 40 mCi (1.5 GBq) of the radioligand was obtained with a specific activity of 200–250 mCi/μmol (7.4–9 GBq/μmol). Chemical (≥96%) and radiochemical purity (≥99%) were determined using analytical HPLC. © 1998 John Wiley & Sons, Ltd.