Abstract：Objective: To research and synthesize the fully automated one-step (11C) labeled water channel protein(AQP) inhibitor, the imaging agent. Materials and Methods: Using the TRACERlab FXC synthesis platform, under 100℃ reaction conditions in alkaline conditions (11C) CH3I reacted with acetazolamide. Then using sodium biphosphate as eluent, through high performance liquid chromatography(HPLC), (11C)N-methylacetazolamide was isolated from reaction solution. Results: The synthesis efficiency of the agent was above 50%, the radiochemical purity was over 98%, the time for the whole producing process was only about 30 min. After intravenous injection of (11C)N-methylacetazolamide into the tail vein of rat, and performing PET/CT scanning, the distribution of the above agent can be seen in rats, after injection of (11C)N-methylacetazolamide and N-methylacetazolamide, the inhibitor, the (11C)N-methylacetazolamide decreased significantly in the rat is liver. Conclusion: This is the first study and report on development of the fully automated one-step (11C) labeled water channel protein(AQP) inhibitor. The (11C)N-methylacetazolamide can be used as AQP PET tracer agent.
2014, Vol. 25 
