Synthesis of [N-methyl-C-11]mianserin: A tetracyclic, atypical antidepressant

As part of our program to develop PET tracers for investigating monoaminerg ic processes in the brain, mianserin, a tetracyclic, atypical antidepressan t, was selected as a candidate for labelling with C-11 for in vivo evaluati on. [N-methyl-C-11]Mianserin was produced by the alkylation of N-desmethyl mianserin with [C-11]methyl iodide followed by HPLC purification and formul ation. [N-methyl-C-11]Mianserin was obtained with a radiochemical. purity > 93% in a 16% decay corrected radiochemical yield. For a typical production starting with 40 GBq [C-11]CO2, 1.9 GBq [N-methyl-C-11]mianserin was obtain ed as a formulated solution in a synthesis time of 35 min (counted from EOB ).