Imaging the 5-HT(1A) receptors with PET: WAY-100635 and analogues.
This paper summarizes our work on WAY-100635 and analogues, labeled either with carbon-11 or fluorine-18, as potential radioligands for the 5-hydroxytryptamine(1A) (5-HT(1A)) neuroreceptors. Other facets of our work include: (1) human studies with [O-methyl-(11)C]WAY-100634, the major radioactive metabolite of [O-methyl-(11)C]WAY-100635, and with [(11)C]CPC 222; (2) use of a human liver metabolism model to screen in vitro potential metabolic problems in humans; (3) modification of the "dry method" to prepare [carbonyl-(11)C]WAY-100635; and (4) validation studies in humans with [carbonyl-(11)C]WAY-100635.
Houle
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S
Vivian M Rakoff PET Centre, Centre for Addiction and Mental Health, Toronto, Canada. shoule@camhpet.on.ca
DaSilva
J N
JN
Wilson
A A
AA
D000818:Animals; D006801:Humans; D008099:Liver / Q000378:metabolism; D010879:Piperazines / Q000378:metabolism*; D010880:Piperidines / Q000378:metabolism; D011725:Pyridines / Q000378:metabolism*; D011985:Receptors, Serotonin / Q000032:analysis*; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists / Q000378:metabolism*; D014055:Tomography, Emission-Computed
C111190:CPC 222; D010879:Piperazines; D010880:Piperidines; D011725:Pyridines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; C090413:N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide