Principles of PET and Its Role in Understanding Drug Delivery to the Brain

  • Stina Syvänen
  • Roger N. Gunn
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 10)


Positron emission tomography (PET) is a non-invasive medical imaging technique that enables the investigation of drug pharmacokinetics in vivo. The technique is especially powerful for pharmacokinetic studies of new CNS drug candidates as tissue samples from the brain are understandably difficult to obtain. The PET technique involves the administration of a radiolabelled molecule whose spatio-temporal distribution can be measured using tomography. The radiolabelled molecule can be the drug under investigation, a structurally different molecule that binds to the same target as the drug candidate or a molecule that interacts with a downstream target that is believed to be affected by the action of the drug candidate. Such radiolabelled probes allow PET to address several questions central for CNS drug development: Does the drug candidate reach the target site? Does the drug candidate interact with the desired target? Is the concentration of the drug at the target site sufficient to illicit an effect? What is the temporal nature of such an interaction? What is the relationship between the target site concentration and the administered dose and/or plasma concentrations?


Positron Emission Tomography Positron Emission Tomography Imaging Positron Emission Tomography Study Receptor Occupancy Positron Emission Tomography Scan 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


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Copyright information

© American Association of Pharmaceutical Scientists 2014

Authors and Affiliations

  1. 1.Department of Public Health and Caring SciencesUppsala UniversityUppsalaSweden
  2. 2.Department of MedicineImperial College LondonLondonUK
  3. 3.Department of Engineering ScienceUniversity of OxfordOxfordUK
  4. 4.ImanovaLondonUK

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