The distribution of [11C]cocaine in normal and cocaine-sensitization mice.
[N-11C-methyl]-cocaine ([11C]cocaine), synthesized by N-methylation of norcocaine with [11C]CH3I, was used to assist in imaging the variety of local distribution by positron emission tomography (PET). The radiochemical yield and the radiochemical purity after purification of [11C]cocaine by high performance liquid chromatography (HPLC) at a sp. act. of 814 GBq/mmol were 47-58% and > 99%, respectively. The time required for synthesis including the purification was 25-30 min from the end of [11C]CH3I trapping. The physical distribution of [11C]cocaine in organ was also investigated in mice at various time after i.v. injection. The main accumulation of radioactivity occurred in the lung, kidney and brain within 1 min after the injection. In the brain, no differences in the organ were observed except the radioactivity level in each section increased for the first 5 min, since then radioactivity decreased dramatically. Furthermore, in the behavioral sensitization model of cocaine, the peak of [11C]cocaine uptake in each brain area was shown to be 5-15 min.
Mizugaki
M
M
Department of Pharmaceutical Sciences, Tohoku University Hospital, Sendai, Japan.
Hishinuma
T
T
Kimura
K
K
Nakamura
H
H
Aso
H
H
Ishii
F
F
Nishikawa
M
M
Itoh
K
K
Tomioka
Y
Y
Ishiwata
S
S
D000818:Animals; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D003042:Cocaine / Q000493:pharmacokinetics* / Q000494:pharmacology; D007668:Kidney / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D051379:Mice; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D003042:Cocaine