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RESEARCH PRODUCT

Positron emission tomography in CNS drug discovery and drug monitoring.

Frank RöschIngo VernalekenMarkus Piel

subject

DrugCentral Nervous Systemmedia_common.quotation_subjectDopamineGlutamic AcidPharmacologyPermeabilityReceptors DopamineDrug DiscoverymedicineAnimalsHumansRadioactive Tracersmedia_commonEnd pointmedicine.diagnostic_testChemistryDrug discoveryDrug candidateTarget engagementBrainModels ChemicalPharmaceutical PreparationsPositron emission tomographyPositron-Emission TomographyReceptors SerotoninSchizophreniaMolecular MedicineMolecular imagingDrug MonitoringGlycolysisBiomedical engineeringCentral Nervous System Agents

description

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.

yearjournalcountryeditionlanguage
2014-09-10Journal of medicinal chemistry
10.1021/jm5001858https://pubmed.ncbi.nlm.nih.gov/25144329