Title:Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging
Volume: 23
Issue: 18
Author(s): Victor W. Pike
Affiliation:
Keywords:
PET, radioligand, molecular imaging, positron-emitter, carbon-11, fluorine-18, efflux transporter,
blood-brain barrier.
Abstract: The development of reversibly binding radioligands for imaging
brain proteins in vivo, such as enzymes, neurotransmitter transporters, receptors
and ion channels, with positron emission tomography (PET) is
keenly sought for biomedical studies of neuropsychiatric disorders and for
drug discovery and development, but is recognized as being highly challenging
at the medicinal chemistry level. This article aims to compile and
discuss the main considerations to be taken into account by chemists embarking
on programs of radioligand development for PET imaging of brain
protein targets.