Synthesis and Evaluation of Mefway Analogs as Ligands for Serotonin 5HT Receptors.

F-Mefway (-{2-[4-(2'-methoxyphenyl)piperazinyl]ethyl}--(2-pyridyl)--(4'-F-fluoro-methylcyclohexane)carboxamide) was developed and evaluated for use as a PET ligand for imaging 5-HT receptors. Ongoing studies of F-Mefway have shown it to be an effective PET radiotracer. We have synthesized isomers of Mefway by changing the position of the methyl-group in attempts to evaluate stability for imaging purposes.

Initial in vivo PET imaging of 5-HT1A receptors with 3-[(18)F]mefway.

4-trans-[(18)F]Mefway is a PET radiotracer with high affinity for 5-HT1A receptors. Our preliminary work indicated the positional isomer, 3-[(18)F]mefway, would be suitable for PET imaging of 5-HT1A receptors. We now compare the in vivo behaviour of 3-mefway with 4-mefway to evaluate 3-[(18)F]mefway as a potential 5-HT1A PET radiotracer.