Table 1 Desired attributes for successful CNS PET ligands
From: Strategies to facilitate the discovery of novel CNS PET ligands
Structure requirements | PK properties |
➢ Structural handle for 18F or 11C labeling | ➢ Brain permeable |
➢ Amenable for late-stage radiolabeling | ➢ No brain permeable radioactive metabolites |
Pharmacology | ➢ Low non-specific binding (NSB) |
➢ Occupy the same binding site for the clinical drug candidate | Safety |
➢ High potency (typically low single digit nM to sub-nM) | ➢ Safe for clinical dosing, typically at μg scale |
➢ High selectivity | ➢ Microdosing GLP: single species IV + 14 day observation |