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Synthesis of [ 18 F] SR144385: a selective radioligand for positron emission tomographic studies of brain cannabinoid receptors
Author(s) -
Mathews William B.,
Ravert Hayden T.,
Musachio John L.,
Frank Richard A.,
RinaldiCarmona Murielle,
Barth Francis,
Dannals Robert F.
Publication year - 1999
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(199906)42:6<589::aid-jlcr219>3.0.co;2-b
Subject(s) - radiosynthesis , chemistry , radioligand , cannabinoid , radiochemistry , cannabinoid receptor , yield (engineering) , fluoride , potassium fluoride , fluorine , nucleophilic substitution , positron emission tomography , antagonist , receptor , medicinal chemistry , organic chemistry , nuclear medicine , biochemistry , inorganic chemistry , medicine , materials science , metallurgy
A cannabinoid receptor antagonist, SR144385, has been labeled with fluorine‐18. [ 18 F] SR144385 was synthesized in a multi‐step reaction in which fluorine‐18 was introduced by nucleophilic halogen displacement on a bromo precursor. The fluorine‐18 labeled intermediate was deprotected and coupled with 1‐aminopiperidine to give [ 18 F]SR144385. The time for radiosynthesis, HPLC purification, and formulation was 2 hours from end‐of‐bombardment. [ 18 F] SR144385 of high radiochemical purity was obtained at end‐of‐synthesis with an average (n=11) specific radioactivity of 1852 mCi/μmol and an average isolated, non‐decay corrected radiochemical yield of 4% from potassium [ 18 F] fluoride. Copyright © 1999 John Wiley & Sons, Ltd.