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The synthesis of [ o‐methyl ‐ 11 C]venlafaxine: A non‐classical, fast‐acting antidepressant
Author(s) -
Gee A. D.,
Smith D. F.,
Gjedde A.
Publication year - 1997
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(199701)39:1<89::aid-jlcr944>3.0.co;2-l
Subject(s) - venlafaxine , chemistry , methyl iodide , antidepressant , radiochemistry , reuptake inhibitor , yield (engineering) , desmethyl , medicinal chemistry , serotonin , biochemistry , medicine , metabolite , materials science , hippocampus , metallurgy , receptor
As part of our program to develop PET tracers for the 5‐HT reuptake site, venlafaxine, a non‐classical, fast‐acting antidepressant, was selected as a candidate for labelling with 11 C for in vivo evaluation. [ O‐methyl ‐ 11 C]venlafaxine was produced by the alkylation of O‐desmethyl venlafaxine with [ 11 C]methyl iodide followed by HPLC purification and formulation. Radiochemically pure [ O‐methyl ‐ 11 C]venlafaxine was obtained in a 30 ± 5 % decay corrected radiochemical yield and a specific activity > 50 GBq / μmol (1.4 Ci / μmol) at the end of synthesis. For a typical production starting with 46 GBq (1.3 Ci) [ 11 C]CO 2 , 5.2 GBq (140 mCi) [ O‐methyl ‐ 11 C]venlafaxine was obtained as a sterile, formulated solution in a synthesis time of 30 min (counted from EOB). © 1997 John Wiley & Sons, Ltd.