PET Quantification of Receptor Occupancy

The use of PET imaging to detect and quantify receptor occupancy (RO) has become a translational standard in CNS discovery and clinical trials. For example, 18F radiolabeling of targeted small molecules enables a PET tracer-based PD biomarker. The tracer can be used for dynamic, non-invasive quantification of percentage RO.

For relevant targets, rodent models can be used to quickly and efficiently:

  • Screen for specificity
  • Validate the target using a cold blocking compound
  • Generate a full dose-RO curve
  • Compare candidate molecules
  • Promising molecules can then be more confidently selected for NHP and/or first in human studies. This inherently also allows quantification of RO, and correlation with efficacy in future translational work.

Please contact us to access the power of PET imaging in CNS discovery.

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