Neuroreceptor PET radioligand development - some basics exemplified by 5-HT1A receptor radioligands Vic Pike Bethesda

The process of developing an effective PET radioligand for imaging a specific brain neurotransmitter receptor is highly challenging. A clinically relevant receptor is normally chosen as the target for PET imaging, which must exist in adequate regional brain concentrations for potential imaging and measurement. Candidate radioligands must minimally meet a wide array of criteria, based on their chemical, physicochemical, pharmacological, pharmacokinetic, pharmacodynamic and metabolic properties.  Hence, very often several radioligand candidates need to be assessed, of which only a very few may turn out to be successful.  Basic considerations in neuroreceptor PET radioligand development will be exemplified by an overview of experience in the development of various radioligands for imaging the brain 5-HT1A receptor.