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Labelling of a new serotoninergic ligand : [ 18 F]ritanserin
Author(s) -
Crouzel C.,
Venet N.,
Sanz G.,
Denis A.
Publication year - 1988
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/jlcr.2580250804
Subject(s) - ritanserin , chemistry , labelling , radiochemistry , radiosynthesis , ligand (biochemistry) , desmethyl , ketone , serotonergic , stereochemistry , medicinal chemistry , nuclear medicine , positron emission tomography , receptor , metabolite , organic chemistry , serotonin , medicine , biochemistry
Ritanserin has been labelled with 18 F to visualize the serotoninergic receptors by Positron Emission Tomography (PET). The synthesis was carried out by a nucleophilic substitution of a nitro substituent of a nitrophenylketone by 18 F − and then addition of a Grignard reagent to the ketone followed by dehydration of the tertiary alcohol so formed. The total time to have [ 18 F]ritanserin ready for injection into a patient was 150 minutes (after the end of bombardement for the 18 F production [ 18 O (p,n) 18 F]). The labelling technique described was used to obtain 1.1 to 1.5 GBq (30 to 40 mCi) of [ 18 F]Ritanserin with a specific activity of 44 GBq/μmol (1.2 Ci/μmol) starting from 18.5 GBq (500 mCi) 18 F.