Journal
NUCLEAR MEDICINE AND BIOLOGY
Volume 27, Issue 5, Pages 441-447Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/S0969-8051(00)00109-8
Keywords
5-HT1A receptors; PET; carbon-11; WAY-100635; CPC-222; FEC; FPC; p-MPPF; NAD-299
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An outline is given of the developments that led to the identification of [O-methyl-C-11]WAY-100635 (4) as the first useful PET ligand for imaging serotonin(1A) (5-HT1A) receptors in the living human brain. Recent attempts to develop 5-HT1A receptor radioligands superior to 4 are reviewed, and [carbonyl[C-11]WAY-100635 (6) has been shown to be the best currently available radioligand for human studies. Of other C-11-radiolabelled compounds, [O-methyl-C-11](R,S)-CPC-222 (9), DWAY (8), and [C-11]NAD-299 (14) all demonstrate specific binding to 5-HT1A receptors in animals and warrant further expedited studies in humans. The trans-fluorocyclohexane, 12, and fluorobenzene, [F-18]p-MPPF 13, are highlighted as examples of promising F-18-labelled ligands. NUCL MED BIOL 27;5:441-447, 2000, (C) 2000 Elsevier Science Inc. All rights reserved.
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