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- W2002193318 abstract "The cocaine congener 2β-carbomethoxy-3β-(4’-iodophenyl)tropane (β-CIT) has a chemical structure that enables labelling with carbon-11 either by N-methylation or by O-methylation. The regional brain uptake of [N-methyl-11C]β-CIT and [O-methyl-11C]β-CIT was compared in cynomolgus monkeys using positron emission tomography (PET). The striatal uptake of radioactivity after intravenous injection of [O-methyl-11C]β-CIT reached a plateau at 30–40 min, whereas the uptake of [N-methyl-11C]β-CIT increased continuously during the time of the PET measurement. Two of the putative labelled metabolites, [N-methyl-11C]β-CIT-acid and [O-methyl-11C]nor-β-CIT were prepared and examined with PET to investigate if they may enter the brain and thus add to the radioactivity uptake obtained with [11C]β-CIT. Less than 0.4% of injected [N-methyl-11C]β-CIT-acid entered the brain whereas 5–6% of [O-methyl-11C]nor-β-CIT entered the brain and accumulated in the striatum and in the thalamus. The fraction of [O-methyl-11C]nor-β-CIT obtained in plasma after intravenous injection of [O-methyl-11C]nor-β-CIT, however, never exceeded 3%. Consequently, the formation of [N-methyl-11C]β-CIT-acidand [O-methyl-11C]nor-β-CIT cannot be the explanation for the different time–activity curves in the monkey brain demonstrated with [11C]β-CIT labelled in two different positions. An unidentified labelled lipophilic metabolite, detected in monkey plasma after injection of [O-methyl-11C]β-CIT, remains as the only possible explanation for the differences between [N-methyl-11C]β-CIT and [O-methyl-11C]β-CIT." @default.
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- W2002193318 date "1999-05-01" @default.
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- W2002193318 title "Different brain radioactivity curves in a PET study with [11C]β-CIT labelled in two different positions" @default.
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- W2002193318 doi "https://doi.org/10.1016/s0969-8051(98)00111-5" @default.
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