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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