The study of the addiction using positron-labeled cocaine

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A tropane type alkaloid, ^<11>C-labeled cocaine was synthesized by N-methylation of norcocaine with ^<11>CH_3I to the assist in the imaging the variety of local distribution by positron emission tomography (PET). The radiochemical yield and the radiochemical purity after purification of ^<11>C-cocaine by HPLC were 58% and > 99% at a specific activity of 22 Ci/mmol. The organ- and regional-distribution of ^<11>C-cocaine was investigated in mice at various times after i. v. injection and we obtained the results of the distribution of ^<11>C-cocaine as follows.1) The accumulation of radioactivity was in the lung, the kidney, the liver and the small intestine.2) No regional differences was observed in the ^<11>C-cocaine uptake in the brain, and the radioactivity level reached the maximum at 5 min. in non-treated mice.3) The sensitization to cocaine delayed the clearance of ^<11>C-cocaine from the brain, the kidney and the stomach.4) In the sensitized model of cocaine, the peaks of ^<11>C-cocainc uptake shifted to 10-15min. after the i. v. injection in most brain regions.5) The pretreatment of cold cocaine did not show the difference of the uptake-pattern of ^<11>C-cocaine in brain.Our present results clarified some differences existed in the localization of there drugs in sensitization models. Such variations may play important roles in the stimulant-derived psychosis.