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In vivo  labelling of serotonergic receptors (5HT) could be a useful tool for understanding the physiological and pathophysiological role of neurodegenerative disorders. 1-[2,5-Dimethoxy-4-iodophenyl]-2-aminopropane (DOI), a well known agonist with high affinity to 5HT 2  receptors, was labelled with C-11 for PET. Here we report the evaluation of the mono-methylated and dimethylated analogs of DOI for PET. The syntheses of [N- 11 C-methyl]-DOI ([ 11 C]MDOI) and [N- 11 C-dimethyl]-DOI ([ 11 C]DMDOI) were optimized resulting in radiochemical yields of up to 43%, allowing efficient production for clinical use. High affinities for the 5HT 2A  and 5HT 2C  receptors with a slight preference for 5HT 2A  were found for MDOI, similar to the highly potent hallucinogen DOI.

Radiosynthesis and in vitro evaluation of the 5HT 2 receptor ligand [N- 11 C-methyl]-1-[2,5-dimethoxy-4-iodophenyl]-2-methylaminopropane for PET