The development of additional radioligands of varying pharmacokinetics for the 5‐HT 1A receptor

Six compounds have been prepared to further probe the structure activity relationships based on the 5‐HT 1A receptor ligand, WAY 100635. The goal is to obtain a series of radiotracers with varying pharmacokinetic properties. Substitution of a pyrimidine for a pyridine moiety, increased the specific binding ratio in the phenylcarboxamide series, but decreased the ratio in the cyclohexanecarboxamide series. A series of compounds with varying pharmacokinetic properties are now available to study a range of properties involving 5‐HT 1A receptor binding.