title: Positron emission tomography in CNS drug discovery and drug monitoring.
abstract: Molecular imaging methods such as positron emission tomography (PET) are increasingly involved in the development of new drugs. Using radioactive tracers as imaging probes, PET allows the determination of the pharmacokinetic and pharmacodynamic properties of a drug candidate, via recording target engagement, the pattern of distribution, and metabolism. Because of the noninvasive nature and quantitative end point obtainable by molecular imaging, it seems inherently suited for the examination of a pharmaceutical's behavior in the brain. Molecular imaging, most especially PET, can therefore be a valuable tool in CNS drug research. In this Perspective, we present the basic principles of PET, the importance of appropriate tracer selection, the impact of improved radiopharmaceutical chemistry in radiotracer development, and the different roles that PET can fulfill in CNS drug research.
authors.affiliation: Institute of Nuclear Chemistry, Johannes Gutenberg-University , Fritz-Strassmann-Weg 2, D-55128 Mainz, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Piel
authors.forename: Ingo
authors.initials: I
authors.lastname: Vernaleken
authors.forename: Frank
authors.initials: F
authors.lastname: Rösch
mesh_terms: D000818:Animals; D001921:Brain / Q000187:drug effects; D002490:Central Nervous System / Q000187:drug effects*; D002491:Central Nervous System Agents / Q000494:pharmacology; D004298:Dopamine / Q000737:chemistry; D055808:Drug Discovery; D016903:Drug Monitoring / Q000379:methods*; D018698:Glutamic Acid / Q000737:chemistry; D006019:Glycolysis; D006801:Humans; D008956:Models, Chemical; D010539:Permeability; D004364:Pharmaceutical Preparations; D049268:Positron-Emission Tomography / Q000379:methods*; D011849:Radioactive Tracers; D011954:Receptors, Dopamine / Q000737:chemistry; D011985:Receptors, Serotonin / Q000737:chemistry; D012559:Schizophrenia / Q000188:drug therapy
chemical_list: D002491:Central Nervous System Agents; D004364:Pharmaceutical Preparations; D011849:Radioactive Tracers; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D018698:Glutamic Acid; D004298:Dopamine