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Synthesis of [ 18 F]phencyclidines for glutamate receptor mapping
Author(s) -
Van Dort M.E.,
Yang D.J.,
Kilbourn M.R.,
Gole D.J.,
Kalir A.,
Domino E.F.,
Young A.B.,
Wieland D.M.
Publication year - 1989
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.25802601150
Subject(s) - tel aviv , humanities , library science , art , computer science
PCP-like potency; 2) developing rapid synthetic methods for incorporating 18F (t% = 110 min) into these compounds for use in in vivo mapping of the glutamate receptor complex by PET. We have shown that 3-a&1o-4-fluoroPCP (2) retains the high binding affinity and pharmaco ogical potency of 3-aminoPCP (2): IC50-300 and 200 nM, respectively, in the 4H-TCP competitive binding assay and ED50t4.48 and 4.55 p/mol/kg, respectively, in the mouse platform test. The synthesis of 4-[18FJfluoro-3-aminoPCP (6) was achieved by nucleophilic displacement of bromide in 4-bromo-3-nitroPCP (4) by nca [ 18F]fluoride ion, followed by reduction of the nitro intermediat (5) with stannous chloride/HCl. In a typi a1 synthesis 22 mCi of [f8F]Tluoride affords 0.60 mCi (EOS) of 4-[1gF]fluoro-3-aminoPCP in a synthesis time of 115 min. Purification was achieved by reverse-phase HPLC. Biological evaluation of this new fluorine-18 ligand is in progress.